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Pseudomonas aeruginosa Quorum Sensing Systems as Drug Discovery Targets: Current Position and Future Perspectives.EBI
J Med Chem 61: 10385-10402 (2018)
University of Nottingham
Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition.EBI
J Med Chem 61: 7065-7086 (2018)
Washington State University
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.EBI
J Med Chem 61: 6869-6891 (2018)
Ube Industries
Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model.EBI
J Med Chem 61: 6724-6735 (2018)
TBA
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets.EBI
J Med Chem 61: 6830-6845 (2018)
University of California San Francisco
25 S-Adamantyl-23-yne-26,27-dinor-1?,25-dihydroxyvitamin DEBI
J Med Chem 61: 6658-6673 (2018)
Universidad De Santiago De Compostela
Swinhoeisterols from the South China Sea Sponge Theonella swinhoei.EBI
J Nat Prod 81: 1645-1650 (2018)
Second Military Medical University
Monoacylglycerol Acyltransferase 2 (MGAT2) Inhibitors for the Treatment of Metabolic Diseases and Nonalcoholic Steatohepatitis (NASH).EBI
J Med Chem 61: 9879-9888 (2018)
TBA
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.EBI
J Med Chem 61: 9791-9810 (2018)
Seoul National University
Antiplasmodial activity of hydroxyethylamine analogs: Synthesis, biological activity and structure activity relationship of plasmepsin inhibitors.EBI
Bioorg Med Chem 26: 3837-3844 (2018)
University of Delhi
Polysaccharide deacetylases serve as new targets for the design of inhibitors against Bacillus anthracis and Bacillus cereus.EBI
Bioorg Med Chem 26: 3845-3851 (2018)
Foundation For Research& Technology-Hellas
The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections.EBI
Bioorg Med Chem 26: 4145-4152 (2018)
Jishou University
Synthesis and biological properties of aryl methyl sulfones.EBI
Bioorg Med Chem 26: 4113-4126 (2018)
Universitat De Barcelona
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.EBI
Bioorg Med Chem Lett 28: 2599-2604 (2018)
China Pharmaceutical University
Inducing protein-protein interactions with molecular glues.EBI
Bioorg Med Chem Lett 28: 2585-2592 (2018)
Pfizer
Macrophilones from the Marine Hydroid Macrorhynchia philippina Can Inhibit ERK Cascade Signaling.EBI
J Nat Prod 81: 1666-1672 (2018)
National Cancer Institute
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.EBI
J Med Chem 61: 5988-6001 (2018)
Zhengzhou University
Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE).EBI
J Med Chem 61: 5934-5948 (2018)
Florida Institute of Technology
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.EBI
Bioorg Med Chem Lett 28: 2605-2610 (2018)
Purdue University
Natural Inhibitors of the RhoA-p115 Complex from the Bark of Meiogyne baillonii.EBI
J Nat Prod 81: 1610-1618 (2018)
Universit£
Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design.EBI
J Med Chem 61: 7573-7588 (2018)
University of Maryland
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI
J Med Chem 61: 9811-9840 (2018)
Universitaire Vaudois
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.EBI
J Med Chem 61: 6937-6943 (2018)
Iqog, Csic
De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors.EBI
J Med Chem 61: 7486-7502 (2018)
Abbvie
Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.EBI
J Med Chem 62: 46-59 (2019)
TBA
Design, synthesis, inávitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors.EBI
Eur J Med Chem 155: 905-924 (2018)
Anadolu University
Deciphering the Inhibition of the Neuronal Calcium Sensor 1 and the Guanine Exchange Factor Ric8a with a Small Phenothiazine Molecule for the Rational Generation of Therapeutic Synapse Function Regulators.EBI
J Med Chem 61: 5910-5921 (2018)
Biological Research Center
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.EBI
J Med Chem 61: 6236-6246 (2018)
Janssen Infectious Diseases-Diagnostics
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.EBI
J Med Chem 61: 6379-6397 (2018)
Shandong University
Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX.EBI
J Med Chem 61: 6328-6338 (2018)
University of Florence
Design, synthesis, and biological evaluation of novel oxadiazole- and thiazole-based histamine HEBI
Bioorg Med Chem 26: 4034-4046 (2018)
Heinrich Heine University D£Sseldorf
Design, synthesis and evaluation of novel bivalent ?-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease.EBI
Bioorg Med Chem 26: 3812-3824 (2018)
China Pharmaceutical University
Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells.EBI
Eur J Med Chem 155: 880-888 (2018)
Cnrs/University of Strasbourg
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGluEBI
Bioorg Med Chem Lett 28: 2641-2646 (2018)
Vanderbilt University
Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease.EBI
Eur J Med Chem 155: 839-846 (2018)
Laboratory of Medicinal Chemistry (Iqog, Csic)
X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.EBI
Eur J Med Chem 155: 806-823 (2018)
West China School of Pharmacy
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.EBI
Bioorg Med Chem 26: 3958-3966 (2018)
Tsinghua University
Design, synthesis and biological evaluation of nitric oxide releasing derivatives of dapagliflozin as potential anti-diabetic and anti-thrombotic agents.EBI
Bioorg Med Chem 26: 3947-3952 (2018)
Guangdong Pharmaceutical University
Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.EBI
J Med Chem 61: 6178-6192 (2018)
Stanford University
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.EBI
J Med Chem 61: 6518-6545 (2018)
Universidad De Oviedo-Principado De Asturias
Exploration of Benzothiazole Rhodacyanines as Allosteric Inhibitors of Protein-Protein Interactions with Heat Shock Protein 70 (Hsp70).EBI
J Med Chem 61: 6163-6177 (2018)
University of California At San Francisco
Discovery of a Potent, Orally Bioavailable PI4KIII? Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo.EBI
J Med Chem 61: 6705-6723 (2018)
Ucb Pharma
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).EBI
Bioorg Med Chem Lett 28: 2636-2640 (2018)
National University of Singapore
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Bioorg Med Chem Lett 28: 2616-2621 (2018)
Vertex Pharmaceuticals
Design, synthesis and pharmacology of aortic-selective acyl-CoA: Cholesterol O-acyltransferase (ACAT/SOAT) inhibitors.EBI
Bioorg Med Chem 26: 4001-4013 (2018)
Kowa
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3K?/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.EBI
Bioorg Med Chem 26: 3992-4000 (2018)
Nanjing University of Chinese Medicine
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.EBI
J Med Chem 61: 6779-6800 (2018)
Pfizer
Izenamides A and B, Statine-Containing Depsipeptides, and an Analogue from a Marine Cyanobacterium.EBI
J Nat Prod 81: 1673-1681 (2018)
Keio University
Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II.EBI
Bioorg Med Chem 26: 4014-4024 (2018)
Martin-Luther-University Halle-Wittenberg
Synthesis and biological evaluations of marine oxohexadecenoic acids: PPAR?/? dual agonism and anti-diabetic target gene effects.EBI
Eur J Med Chem 155: 736-753 (2018)
University of Oslo
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFEBI
Eur J Med Chem 155: 725-735 (2018)
Nanjing University
5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.EBI
Eur J Med Chem 155: 714-724 (2018)
Shandong University
Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.EBI
J Med Chem 61: 6350-6363 (2018)
University of California Riverside
Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-?B Inducing Kinase.EBI
J Med Chem 61: 6801-6813 (2018)
Genentech
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.EBI
J Med Chem 61: 6056-6074 (2018)
Second Military Medical University
Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice.EBI
J Med Chem 61: 6075-6086 (2018)
TBA
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.EBI
J Med Chem 61: 9841-9878 (2018)
Shanghaitech University
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.EBI
J Med Chem 61: 6034-6055 (2018)
University of Turin
Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity.EBI
J Med Chem 61: 6140-6152 (2018)
University of Salerno
Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling.EBI
ACS Med Chem Lett 9: 563-568 (2018)
The Scripps Research Institute
Chemical Proteomic Characterization of a Covalent KRASG12C Inhibitor.EBI
ACS Med Chem Lett 9: 557-562 (2018)
Lilly Research Laboratories
Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.EBI
ACS Med Chem Lett 9: 546-551 (2018)
Promega
Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.EBI
ACS Med Chem Lett 9: 540-545 (2018)
Dana-Farber Cancer Institute
Expansion of cat-ELCCA for the Discovery of Small Molecule Inhibitors of the Pre-let-7-Lin28 RNA-Protein Interaction.EBI
ACS Med Chem Lett 9: 517-521 (2018)
University of Michigan
Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3K? inhibitors.EBI
Bioorg Med Chem 26: 3982-3991 (2018)
Shenyang Pharmaceutical University
Identification of the Histidine Residue in Vitamin D Receptor That Covalently Binds to Electrophilic Ligands.EBI
J Med Chem 61: 6339-6349 (2018)
Showa Pharmaceutical University
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.EBI
Eur J Med Chem 155: 695-704 (2018)
The University of Queensland
Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy.EBI
Bioorg Med Chem Lett 28: 2655-2659 (2018)
Mitobridge, Inc. (An Astellas)
Discovery of a novel 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EPEBI
Bioorg Med Chem Lett 28: 2408-2412 (2018)
Asahi Kasei Pharma
Design and synthesis of selenazole-substituted ritonavir analogs.EBI
Bioorg Med Chem Lett 28: 2379-2381 (2018)
Chinese Academy of Science
Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAFEBI
Bioorg Med Chem Lett 28: 2382-2390 (2018)
Nanjing University
Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors.EBI
Bioorg Med Chem 26: 3953-3957 (2018)
University of Salerno
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies.EBI
Bioorg Med Chem 26: 3975-3981 (2018)
Nanjing Forestry University
Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism.EBI
J Med Chem 61: 5949-5962 (2018)
Chugai Pharmaceutical
An imidazole based H-Phe-Phe-NHEBI
Bioorg Med Chem Lett 28: 2446-2450 (2018)
Uppsala University
Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors.EBI
J Med Chem 61: 6277-6292 (2018)
Vichem Chemie Research
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.EBI
J Med Chem 61: 6087-6109 (2018)
Chinese Academy of Medical Sciences and Peking Union Medical College
Selective inhibition of monoamine oxidase A by chelerythrine, an isoquinoline alkaloid.EBI
Bioorg Med Chem Lett 28: 2403-2407 (2018)
Sunchon National University
Development of New Photoswitchable Azobenzene Based ?-Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation.EBI
J Med Chem 61: 6211-6235 (2018)
Ludwig-Maximilians-University Munich
The mimics of NEBI
Bioorg Med Chem Lett 28: 2375-2378 (2018)
School of Pharmacy
Lung cancer and matrix metalloproteinases inhibitors of polyphenols from Selaginella tamariscina with suppression activity of migration.EBI
Bioorg Med Chem Lett 28: 2413-2417 (2018)
Guangxi Normal University
Design, synthesis and bioevaluation of 2-mercapto-6-phenylpyrimidine-4-carboxylic acid derivatives as potent xanthine oxidase inhibitors.EBI
Eur J Med Chem 155: 590-595 (2018)
Shenyang Pharmaceutical University
Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.EBI
J Med Chem 61: 6308-6327 (2018)
TBA
Rational design of novel irreversible inhibitors for human arginase.EBI
Bioorg Med Chem 26: 3939-3946 (2018)
Brown University
4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors.EBI
J Med Chem 61: 5765-5770 (2018)
Universit£
Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.EBI
Bioorg Med Chem Lett 28: 2436-2441 (2018)
Yeungnam University
Spiro[pyrrolidine-3,3'-oxindoles] as 5-HTEBI
Bioorg Med Chem Lett 28: 2418-2421 (2018)
Hungarian Academy of Sciences
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.EBI
J Med Chem 61: 5974-5987 (2018)
Astrazeneca
Identification of fused pyrimidines as interleukin 17 secretion inhibitors.EBI
Eur J Med Chem 155: 562-578 (2018)
Norwegian University of Science and Technology
Structure-activity relationship studies and pharmacological characterization of NEBI
Eur J Med Chem 155: 552-561 (2018)
Universit£
Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors.EBI
Eur J Med Chem 155: 545-551 (2018)
Kurukshetra University
Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.EBI
NA
University of Catania
Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials.EBI
NA
Universita Degli Studi Di Siena
Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position.EBI
Eur J Med Chem 155: 428-433 (2018)
University of Perugia
Optimization and in vivo evaluation of pyrazolopyridines as a potent and selective PI3K? inhibitor.EBI
Bioorg Med Chem 26: 3917-3924 (2018)
Astellas Pharma
The tyrosinase inhibitory effects of isoxazolone derivatives with a (Z)-?-phenyl-?, ?-unsaturated carbonyl scaffold.EBI
Bioorg Med Chem 26: 3882-3889 (2018)
Pusan National University
Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).EBI
J Med Chem 61: 6247-6260 (2018)
Janssen Pharmaceutical Companies of Johnson & Johnson
Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.EBI
J Med Chem 61: 5609-5622 (2018)
East China University of Science and Technology
Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy.EBI
Bioorg Med Chem Lett 28: 2498-2503 (2018)
Shionogi
Synthesis, in vitro and in silico studies of novel potent urease inhibitors: N-[4-({5-[(3-Un/substituted-anilino-3-oxopropyl)sulfanyl]-1,3,4-oxadiazol-2-yl}methyl)-1,3-thiazol-2-yl]benzamides.EBI
Bioorg Med Chem 26: 3791-3804 (2018)
Kongju National University
Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity.EBI
Bioorg Med Chem 26: 5349-5358 (2018)
University of Alberta
Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18.EBI
Eur J Med Chem 155: 381-397 (2018)
University of Bonn
Structure-based discovery of selective BRPF1 bromodomain inhibitors.EBI
Eur J Med Chem 155: 337-352 (2018)
University of Zurich
Surmounting the resistance against EGFR inhibitors through the development of thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors.EBI
Eur J Med Chem 155: 316-336 (2018)
Ain Shams University
Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics.EBI
J Med Chem 61: 5442-5447 (2018)
Swiss Federal Institute of Technology (Eth)
Constraining Endomorphin-1 by ?,?-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel ?-Opioid Receptor Selective Partial Agonist.EBI
J Med Chem 61: 5751-5757 (2018)
University of Bologna
Discovery of the selective and efficacious inhibitors of FLT3 mutations.EBI
Eur J Med Chem 155: 303-315 (2018)
China Pharmaceutical University
Investigation of synergistic antimicrobial effects of the drug combinations of meropenem and 1,2-benzisoselenazol-3(2H)-one derivatives on carbapenem-resistant Enterobacteriaceae producing NDM-1.EBI
Eur J Med Chem 155: 285-302 (2018)
The Hong Kong Polytechnic University
Sterol 14?-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.EBI
J Med Chem 61: 5679-5691 (2018)
Vanderbilt University School of Medicine
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.EBI
J Med Chem 61: 6546-6573 (2018)
Wuxi Apptec (Tianjin) Co.
Rational design of mitochondria-targeted pyruvate dehydrogenase kinase 1 inhibitors with improved selectivity and antiproliferative activity.EBI
Eur J Med Chem 155: 275-284 (2018)
Chongqing University
Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.EBI
J Med Chem 61: 5692-5703 (2018)
University of Cape Town
Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.EBI
J Med Chem 61: 5623-5642 (2018)
TBA
Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists.EBI
Bioorg Med Chem 26: 3716-3726 (2018)
Astellas Pharma
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.EBI
Bioorg Med Chem Lett 28: 2481-2484 (2018)
Fr£Res Mentouri-Constantine University
Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.EBI
J Med Chem 61: 6018-6033 (2018)
Dart Neuroscience
Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).EBI
Eur J Med Chem 155: 229-243 (2018)
University of Genoa
Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRAFEBI
Eur J Med Chem 155: 210-228 (2018)
Southern Medical University
Design, synthesis, structure-activity relationships study and X-ray crystallography of 3-substituted-indolin-2-one-5-carboxamide derivatives as PAK4 inhibitors.EBI
Eur J Med Chem 155: 197-209 (2018)
Shenyang Pharmaceutical University
Rational design of carbamate-based dual binding site and central AChE inhibitors by a "biooxidisable" prodrug approach: Synthesis, inávitro evaluation and docking studies.EBI
Eur J Med Chem 155: 171-182 (2018)
Cnrs
Synthesis, structure-activity relationship and molecular docking studies of 3-O-flavonol glycosides as cholinesterase inhibitors.EBI
Bioorg Med Chem 26: 3696-3706 (2018)
University of Gujrat
Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors.EBI
Bioorg Med Chem 26: 3668-3687 (2018)
Ludwig-Maximilians-Universit£T M£Nchen
Synthesis and biological evaluation of curcumin derivatives modified with ?-amino boronic acid as proteasome inhibitors.EBI
Bioorg Med Chem Lett 28: 2459-2464 (2018)
Peking University
Design, synthesis, molecular modeling and anti-proliferative evaluation of novel quinoxaline derivatives as potential DNA intercalators and topoisomerase II inhibitors.EBI
Eur J Med Chem 155: 117-134 (2018)
Al-Azhar University
Structure-based drug design to overcome species differences in kallikrein 7 inhibition of 1,3,6-trisubstituted 1,4-diazepan-7-ones.EBI
Bioorg Med Chem 26: 3639-3653 (2018)
Asubio Pharma
Synthesis of sulfadiazinyl acyl/aryl thiourea derivatives as calf intestinal alkaline phosphatase inhibitors, pharmacokinetic properties, lead optimization, Lineweaver-Burk plot evaluation and binding analysis.EBI
Bioorg Med Chem 26: 3707-3715 (2018)
Quaid-I-Azam University
Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.EBI
Bioorg Med Chem Lett 28: 2539-2542 (2018)
Seoul National University
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to ?EBI
J Med Chem 61: 7474-7485 (2018)
Irccs Ospedale San Raffaele
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.EBI
J Med Chem 61: 5643-5663 (2018)
Hospitales Universitarios De Granada/University of Granada
Integrated Strategy for Lead Optimization Based on Fragment Growing: The Diversity-Oriented-Target-Focused-Synthesis Approach.EBI
J Med Chem 61: 5719-5732 (2018)
Aix-Marseille University
Characterizing hydration sites in protein-ligand complexes towards the design of novel ligands.EBI
Bioorg Med Chem Lett 28: 2343-2352 (2018)
Sanofi-Aventis Deutschland
1,2-Diphenoxiethane salts as potent antiplasmodial agents.EBI
Bioorg Med Chem Lett 28: 2485-2489 (2018)
Universidad De Granada
Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human AEBI
Bioorg Med Chem 26: 3688-3695 (2018)
Universit£
Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.EBI
J Med Chem 61: 5580-5593 (2018)
Sanofi-Aventis Deutschland
Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.EBI
J Med Chem 61: 5594-5608 (2018)
Mitsubishi Tanabe Pharma
Total Syntheses of Lobaric Acid and Its Derivatives from the Antarctic Lichen Stereocaulon alpinum.EBI
J Nat Prod 81: 1460-1467 (2018)
Korea Polar Research Institute
Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.EBI
J Med Chem 61: 5758-5764 (2018)
Goethe University Frankfurt
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.EBI
J Med Chem 61: 5704-5718 (2018)
Pfizer
Medicinal Chemistry and Use of Myosin II Inhibitor ( S)-Blebbistatin and Its Derivatives.EBI
J Med Chem 61: 9410-9428 (2018)
Ghent University
Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.EBI
J Med Chem 61: 5412-5423 (2018)
TBA
Druggability Assessment of Targets Used in Kinetic Target-Guided Synthesis.EBI
J Med Chem 61: 9395-9409 (2018)
University of Groningen
Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.EBI
Bioorg Med Chem Lett 28: 2477-2480 (2018)
The Ohio State University
Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.EBI
Bioorg Med Chem Lett 28: 2513-2517 (2018)
Keimyung University
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.EBI
Eur J Med Chem 155: 96-116 (2018)
Celon Pharma
Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches.EBI
J Med Chem 61: 8947-8980 (2018)
Shandong University
Demonstration of In Vitro Resurrection of Aged Acetylcholinesterase after Exposure to Organophosphorus Chemical Nerve Agents.EBI
J Med Chem 61: 7034-7042 (2018)
The Ohio State University-Marion
Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery.EBI
J Med Chem 61: 9429-9441 (2018)
Sun Yat-Sen University
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.EBI
J Med Chem 61: 9030-9058 (2018)
Genentech
Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties.EBI
J Med Chem 61: 5881-5899 (2018)
University of Colorado
Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist.EBI
J Nat Prod 81: 1343-1356 (2018)
Seoul National University
Identification of quinone analogues as potential inhibitors of picornavirus 3C protease in vitro.EBI
Bioorg Med Chem Lett 28: 2533-2538 (2018)
Korea Research Institute of Chemical Technology
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.EBI
Bioorg Med Chem 26: 3076-3095 (2018)
Alzahra University
Synthesis, molecular modelling studies and biological evaluation of new oxoeicosanoid receptor 1 agonists.EBI
Bioorg Med Chem 26: 3580-3587 (2018)
Hospital Del Mar Medical Research Institute (Imim)
Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.EBI
J Med Chem 61: 8078-8087 (2018)
Genentech
Computer-aided discovery and biological characterization of human lactate dehydrogenase 5 inhibitors with anti-osteosarcoma activity.EBI
Bioorg Med Chem Lett 28: 2229-2233 (2018)
Capital Medical University
?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.EBI
J Med Chem 61: 6261-6276 (2018)
Seoul National University
Structure-based lead optimization to improve antiviral potency and ADMET properties of phenyl-1H-pyrrole-carboxamide entry inhibitors targeted to HIV-1 gp120.EBI
Eur J Med Chem 154: 367-391 (2018)
Lindsley F. Kimball Research Institute
Structural basis for the selective inhibition of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) by a selenium-containing inhibitor with chloro-aminopyridine as a basic group.EBI
Bioorg Med Chem Lett 28: 2256-2260 (2018)
Showa Pharmaceutical University
Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry.EBI
Bioorg Med Chem 26: 3145-3157 (2018)
Shandong University
Structure-based design and profiling of novel 17?-HSD14 inhibitors.EBI
Eur J Med Chem 155: 61-76 (2018)
Philipps University Marburg
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.EBI
Bioorg Med Chem 26: 3664-3667 (2018)
University of Arizona
Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and ?-secretase inhibition activities.EBI
Eur J Med Chem 155: 49-60 (2018)
Tehran University of Medical Sciences
Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays.EBI
Eur J Med Chem 155: 34-48 (2018)
Soochow University
Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.EBI
J Med Chem 61: 5367-5379 (2018)
University of Pennsylvania
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.EBI
J Med Chem 61: 5332-5349 (2018)
China Pharmaceutical University
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.EBI
J Med Chem 61: 5235-5244 (2018)
Astrazeneca
Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.EBI
J Med Chem 61: 6002-6017 (2018)
Vanderbilt University
Antitumorigenic Properties of Omega-3 Endocannabinoid Epoxides.EBI
J Med Chem 61: 5569-5579 (2018)
TBA
The recent progress of isoxazole in medicinal chemistry.EBI
Bioorg Med Chem 26: 3065-3075 (2018)
China Pharmaceutical University
Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold.EBI
Bioorg Med Chem 26: 3619-3633 (2018)
Xi'An Jiaotong University
Rational design of bis-indolylmethane-oxadiazole hybrids as inhibitors of thymidine phosphorylase.EBI
Bioorg Med Chem 26: 3654-3663 (2018)
Imam Abdulrahman Bin Faisal University
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.EBI
Bioorg Med Chem 26: 3491-3501 (2018)
Shihezi University
Pyrroloquinoline scaffold-based 5-HTEBI
Bioorg Med Chem 26: 3588-3595 (2018)
Jagiellonian University Medical College
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI
Bioorg Med Chem Lett 28: 2250-2255 (2018)
Universit£
Chemical space screening around PheEBI
Bioorg Med Chem Lett 28: 2320-2323 (2018)
Vrije Universiteit Brussel
Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents.EBI
Eur J Med Chem 155: 13-23 (2018)
Jamia Millia Islamia
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.EBI
J Med Chem 61: 5435-5441 (2018)
Pharmaron-Beijing
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.EBI
J Med Chem 61: 5138-5153 (2018)
Kobe Gakuin University
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.EBI
J Med Chem 61: 5350-5366 (2018)
Eberhard Karls University T£Bingen
Discovery of ?-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.EBI
J Med Chem 61: 5380-5394 (2018)
University of Florence
New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm.EBI
J Med Chem 61: 9004-9029 (2018)
Astrazeneca
Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis.EBI
J Med Chem 61: 8563-8593 (2018)
The Maharaja Sayajirao University of Baroda
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.EBI
J Med Chem 61: 8981-9003 (2018)
China Pharmaceutical University
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase? (PI3K?) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).EBI
J Med Chem 61: 5245-5256 (2018)
Vertex Pharmaceuticals
Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.EBI
Eur J Med Chem 154: 314-323 (2018)
National Taiwan University
Advances and Insights for Small Molecule Inhibition of Macrophage Migration Inhibitory Factor.EBI
J Med Chem 61: 8104-8119 (2018)
Yale University
Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.EBI
J Med Chem 61: 5292-5303 (2018)
Janssen Pharmaceutica
Jizanpeptins, Cyanobacterial Protease Inhibitors from a Symploca sp. Cyanobacterium Collected in the Red Sea.EBI
J Nat Prod 81: 1417-1425 (2018)
Oregon State University
New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting.EBI
Bioorg Med Chem Lett 28: 2289-2293 (2018)
University of Ferrara
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.EBI
Bioorg Med Chem Lett 28: 2566-2572 (2018)
Chungnam National University
Design, synthesis and biological evaluation of phosphopeptides as Polo-like kinase 1 Polo-box domain inhibitors.EBI
Bioorg Med Chem 26: 3429-3437 (2018)
China Pharmaceutical University
Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents.EBI
Eur J Med Chem 154: 253-266 (2018)
School of Pharmaceutical Sciences
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy.EBI
Bioorg Med Chem 26: 3559-3572 (2018)
Shanghai Institute of Materia Medica
Elucidating the inhibition of peptidoglycan biosynthesis in Staphylococcus aureus by albocycline, a macrolactone isolated from Streptomyces maizeus.EBI
Bioorg Med Chem 26: 3453-3460 (2018)
University of Delaware
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.EBI
Bioorg Med Chem Lett 28: 2338-2342 (2018)
Shionogi
SAR studies on truxillic acid mono esters as a new class of antinociceptive agents targeting fatty acid binding proteins.EBI
Eur J Med Chem 154: 233-252 (2018)
Stony Brook University
Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects.EBI
Eur J Med Chem 154: 210-219 (2018)
Universit£
Adamantyl thioureas as soluble epoxide hydrolase inhibitors.EBI
Bioorg Med Chem Lett 28: 2302-2313 (2018)
University of California Davis
Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17?-hydroxylase-C17,20-lyase (Cyp17).EBI
Bioorg Med Chem Lett 28: 2270-2274 (2018)
Temple University
Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective.EBI
Bioorg Med Chem 26: 3438-3452 (2018)
Bharathiar University
Development of novel amino-quinoline-5,8-dione derivatives as NAD(P)H:quinone oxidoreductase 1 (NQO1) inhibitors with potent antiproliferative activities.EBI
Eur J Med Chem 154: 199-209 (2018)
Nantong University
Structure-activity relationship of uridine-based nucleoside phosphoramidate prodrugs for inhibition of dengue virus RNA-dependent RNA polymerase.EBI
Bioorg Med Chem Lett 28: 2324-2327 (2018)
Novartis Institute For Tropical Diseases
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.EBI
J Med Chem 61: 5187-5198 (2018)
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Isoxazole-tethered diarylheptanoid analogs: Discovery of a new drug-like PAR2 antagonist.EBI
Bioorg Med Chem Lett 28: 2285-2288 (2018)
Advinus Therapeutics
Development of autotaxin inhibitors: A series of zinc binding triazoles.EBI
Bioorg Med Chem Lett 28: 2279-2284 (2018)
Novartis Institutes For Biomedical Research
Cyclic Peptidic Mimetics of Apollo Peptides Targeting Telomeric Repeat Binding Factor 2 (TRF2) and Apollo Interaction.EBI
ACS Med Chem Lett 9: 507-511 (2018)
China Pharmaceutical University
Synthesis and EBI
ACS Med Chem Lett 9: 496-501 (2018)
Vrije Universiteit Brussel
Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D.EBI
ACS Med Chem Lett 9: 490-495 (2018)
Novartis Pharma
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.EBI
ACS Med Chem Lett 9: 472-477 (2018)
Bristol-Myers Squibb Research and Development
Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology.EBI
ACS Med Chem Lett 9: 462-467 (2018)
University of Florence
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.EBI
ACS Med Chem Lett 9: 457-461 (2018)
Merck
Discovery of EBI
ACS Med Chem Lett 9: 446-451 (2018)
Emory University
Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).EBI
ACS Med Chem Lett 9: 440-445 (2018)
Pfizer
Phenotypic Screening To Discover Novel Chemical Series as Efficient Antihemorrhagic Agents.EBI
ACS Med Chem Lett 9: 428-433 (2018)
Universidad De Navarra
SAR Studies of EBI
ACS Med Chem Lett 9: 422-427 (2018)
Chinese Academy of Sciences
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).EBI
ACS Med Chem Lett 9: 417-421 (2018)
Genentech
2,7-Diazaspiro[4,4]nonanes for the Treatment or Prevention of Cancers and Diabetes.EBI
ACS Med Chem Lett 9: 401-402 (2018)
Usona Institute
A comparative study of non-native N-acyl l-homoserine lactone analogs in two Pseudomonas aeruginosa quorum sensing receptors that share a common native ligand yet inversely regulate virulence.EBI
Bioorg Med Chem 26: 5336-5342 (2018)
University of Wisconsin-Madison
Design, synthesis and molecular modeling of new 4-phenylcoumarin derivatives as tubulin polymerization inhibitors targeting MCF-7 breast cancer cells.EBI
Bioorg Med Chem 26: 3474-3490 (2018)
National Research Centre
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.EBI
Eur J Med Chem 154: 155-171 (2018)
University of Bern
Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease.EBI
J Med Chem 61: 5269-5278 (2018)
Uppsala University
Structure-Based Design of Inhibitors with Improved Selectivity for Steroidogenic Cytochrome P450 17A1 over Cytochrome P450 21A2.EBI
J Med Chem 61: 4946-4960 (2018)
University of Kansas
Peniisocoumarins A-J: Isocoumarins from Penicillium commune QQF-3, an Endophytic Fungus of the Mangrove Plant Kandelia candel.EBI
J Nat Prod 81: 1376-1383 (2018)
Sun Yat-Sen University
Antidiabetic potential of phytochemicals isolated from the stem bark of Myristica fatua Houtt. var. magnifica (Bedd.) Sinclair.EBI
Bioorg Med Chem 26: 3461-3467 (2018)
Csir-National Institute For Interdisciplinary Science and Technology
Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.EBI
Eur J Med Chem 154: 144-154 (2018)
Anhui Medical University
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.EBI
J Med Chem 61: 5304-5322 (2018)
Shandong University
Chiral analogues of (+)-cyclazosin as potent?EBI
Bioorg Med Chem 26: 3502-3513 (2018)
Universit£
Boronic acid inhibitors of the class A?-lactamase KPC-2.EBI
Bioorg Med Chem 26: 2921-2927 (2018)
Ucl School of Pharmacy
Potent and Highly Selective Inhibitors of the Proteasome Trypsin-like Site by Incorporation of Basic Side Chain Containing Amino Acid Derived Sulfonyl Fluorides.EBI
J Med Chem 61: 5395-5411 (2018)
University of Glasgow
Synthesis and antiviral evaluation of novel peptidomimetics as norovirus protease inhibitors.EBI
Bioorg Med Chem Lett 28: 2165-2170 (2018)
Emory University
The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.EBI
Bioorg Med Chem Lett 28: 2124-2130 (2018)
Bristol-Myers Squibb Research and Development
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.EBI
Bioorg Med Chem Lett 28: 2159-2164 (2018)
Janssen Research and Development
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.EBI
Bioorg Med Chem 26: 2996-3005 (2018)
University of Liverpool
Specific Stereoisomeric Conformations Determine the Drug Potency of Cladosporin Scaffold against Malarial Parasite.EBI
J Med Chem 61: 5664-5678 (2018)
Csir-National Chemical Laboratory
New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.EBI
Eur J Med Chem 154: 117-132 (2018)
University of Ljubljana
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.EBI
Eur J Med Chem 154: 101-109 (2018)
University of Tours
Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators.EBI
Eur J Med Chem 154: 68-90 (2018)
University of Ljubljana
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.EBI
Bioorg Med Chem 26: 2937-2957 (2018)
University of Oxford
An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated CaEBI
Bioorg Med Chem 26: 3406-3413 (2018)
University of Auckland
Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11.EBI
Bioorg Med Chem Lett 28: 2143-2147 (2018)
Forma Therapeutics
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.EBI
Eur J Med Chem 154: 9-28 (2018)
Chinese Academy of Sciences
From hit to lead: Structure-based discovery of naphthalene-1-sulfonamide derivatives as potent and selective inhibitors of fatty acid binding protein 4.EBI
Eur J Med Chem 154: 44-59 (2018)
Fudan University
Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors.EBI
Eur J Med Chem 154: 29-43 (2018)
Jiangxi Science & Technology Normal University
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine ?-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.EBI
J Med Chem 61: 5525-5546 (2018)
TBA
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.EBI
J Med Chem 61: 4978-4992 (2018)
Astex Pharmaceuticals
Piperidine Alkaloids with Diverse Skeletons from Anacyclus pyrethrum.EBI
J Nat Prod 81: 1474-1482 (2018)
Chinese Academy of Sciences
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.EBI
J Med Chem 61: 4791-4809 (2018)
Universit£
Factor XIa Inhibitors as New Anticoagulants.EBI
J Med Chem 61: 7425-7447 (2018)
Bristol-Myers Squibb
Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds.EBI
J Med Chem 61: 5279-5291 (2018)
University of Liege
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib.EBI
Bioorg Med Chem Lett 28: 2148-2152 (2018)
Fudan University
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.EBI
Bioorg Med Chem Lett 28: 2131-2135 (2018)
Chinese Academy of Sciences
Plasmodial Kinase Inhibitors: License to Cure?EBI
J Med Chem 61: 8061-8077 (2018)
TBA
NMR Biochemical Assay for Oxidosqualene Cyclase: Evaluation of Inhibitor Activities on Trypanosoma cruzi and Human Enzymes.EBI
J Med Chem 61: 5047-5053 (2018)
National Institute of Advanced Industrial Science and Technology (Aist)
Structure-Activity Relationships and Therapeutic Potentials of 5-HTEBI
J Med Chem 61: 8475-8503 (2018)
Universit£
Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.EBI
J Med Chem 61: 4883-4903 (2018)
National Center For Advancing Translational Sciences
Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI
J Med Chem 61: 4860-4882 (2018)
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.EBI
Bioorg Med Chem 26: 3021-3029 (2018)
The Institute of Cancer Research
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.EBI
Bioorg Med Chem 26: 3399-3405 (2018)
Bienta/Enamine
Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases.EBI
Bioorg Med Chem 26: 2984-2991 (2018)
University of Oxford
Synthesis and biological evaluation of 6-hydroxyl C-aryl glucoside derivatives as novel sodium glucose co-transporter 2 (SGLT2) inhibitors.EBI
Bioorg Med Chem Lett 28: 2201-2205 (2018)
Shandong University
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.EBI
Bioorg Med Chem Lett 28: 2195-2200 (2018)
Novartis Institutes For Biomedical Research
Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds.EBI
Eur J Med Chem 152: 600-614 (2018)
Tehran University of Medical Sciences
A review on flavonoid-based scaffolds as multi-target-directed ligands (MTDLs) for Alzheimer's disease.EBI
NA
Tehran University of Medical Sciences
Inhibitors of Melanogenesis: An Updated Review.EBI
J Med Chem 61: 7395-7418 (2018)
University of Bonn
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HTEBI
J Med Chem 61: 4993-5008 (2018)
Suven Life Sciences
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.EBI
J Med Chem 61: 4561-4577 (2018)
Purdue University
Isolation, Synthesis, and Antisepsis Effects of a C-Methylcoumarinochromone Isolated from Abronia nana Cell Culture.EBI
J Nat Prod 81: 1173-1182 (2018)
Kyungpook National University
Novel non-ATP competitive small molecules targeting the CK2 ?/? interface.EBI
Bioorg Med Chem 26: 3016-3020 (2018)
University of Cambridge
N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.EBI
Bioorg Med Chem Lett 28: 2153-2158 (2018)
Novartis Institutes For Biomedical Research
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.EBI
Eur J Med Chem 152: 542-559 (2018)
Chinese Academy of Sciences
The discovery of VU0486846: steep SAR from a series of MEBI
Bioorg Med Chem Lett 28: 2175-2179 (2018)
Vanderbilt University Medical Center
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.EBI
Bioorg Med Chem 26: 3261-3286 (2018)
Takeda Pharmaceutical
Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery.EBI
Eur J Med Chem 152: 489-514 (2018)
Universidad De Navarra
Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines, a promising privileged structure.EBI
Bioorg Med Chem 26: 3296-3307 (2018)
Universities of Lille
Brain penetrant kinase inhibitors: Learning from kinase neuroscience discovery.EBI
Bioorg Med Chem Lett 28: 1981-1991 (2018)
Eli Lilly
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).EBI
Bioorg Med Chem Lett 28: 2222-2227 (2018)
Daiichi Sankyo
Current anti-diabetic agents and their molecular targets: A review.EBI
NA
University of Kwazulu-Natal
Synthesis and biological evaluation of ?EBI
Eur J Med Chem 152: 424-435 (2018)
Shenyang Pharmaceutical University
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for ?EBI
Eur J Med Chem 152: 401-416 (2018)
Istituto Di Chimica Biomolecolare
New developments in non-quinolone-based antibiotics for the inhibiton of bacterial gyrase and topoisomerase IV.EBI
Eur J Med Chem 152: 393-400 (2018)
Islamia College University
Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases.EBI
J Med Chem 61: 8088-8103 (2018)
University of Copenhagen
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.EBI
Bioorg Med Chem 26: 3242-3253 (2018)
Shenyang Pharmaceutical University
Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.EBI
Bioorg Med Chem Lett 28: 2050-2054 (2018)
Mcdaniel College
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.EBI
Bioorg Med Chem Lett 28: 2029-2034 (2018)
Merck
Discovery of (E)-1-amino-4-phenylbut-3-en-2-ol derivatives as novel neuraminidase inhibitors.EBI
Bioorg Med Chem Lett 28: 2003-2007 (2018)
Shanghai Institute of Technology
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.EBI
Bioorg Med Chem Lett 28: 2084-2090 (2018)
West China Hospital
From Cancer to Pain Target by Automated Selectivity Inversion of a Clinical Candidate.EBI
J Med Chem 61: 4851-4859 (2018)
Heidelberg University
Expanding Benzoxazole-Based Inosine 5'-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents.EBI
J Med Chem 61: 4739-4756 (2018)
National Institute of Allergy and Infectious Diseases
Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis.EBI
J Med Chem 61: 4961-4977 (2018)
Ege University Bornova
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.EBI
J Med Chem 61: 4757-4773 (2018)
TBA
Structures of Ebola Virus Glycoprotein Complexes with Tricyclic Antidepressant and Antipsychotic Drugs.EBI
J Med Chem 61: 4938-4945 (2018)
University of Oxford
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.EBI
J Med Chem 61: 4720-4738 (2018)
Concordia University Wisconsin
Identification and Structure-Activity Relationship of HDAC6 Zinc-Finger Ubiquitin Binding Domain Inhibitors.EBI
J Med Chem 61: 4517-4527 (2018)
University of Toronto
Lactam hybrid analogues of solonamide B and autoinducing peptides as potent S.áaureus AgrC antagonists.EBI
Eur J Med Chem 152: 370-376 (2018)
University of Copenhagen
Design and biological evaluation of tetrahydro-?-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors.EBI
Eur J Med Chem 152: 329-357 (2018)
University of Regensburg
Complexity of Blocking Bivalent Protein-Protein Interactions: Development of a Highly Potent Inhibitor of the Menin-Mixed-Lineage Leukemia Interaction.EBI
J Med Chem 61: 4832-4850 (2018)
University of Michigan
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaEBI
J Med Chem 61: 4810-4831 (2018)
Xenon Pharmaceuticals
Discovery of tetrahydroindazoles as a novel class of potent and in vivo efficacious gamma secretase modulators.EBI
Bioorg Med Chem 26: 3227-3241 (2018)
Boehringer Ingelheim Pharma
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.EBI
J Med Chem 61: 4928-4937 (2018)
University of Santiago De Compostela
Rational Design of Novel 1,3-Oxazine Based ?-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust A? Reduction in the Brain.EBI
J Med Chem 61: 5122-5137 (2018)
TBA
Molecular Determinants Conferring the Stoichiometric-Dependent Activity of ?-Conotoxins at the Human ?9?10 Nicotinic Acetylcholine Receptor Subtype.EBI
J Med Chem 61: 4628-4634 (2018)
Ocean University of China
Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ.EBI
Bioorg Med Chem Lett 28: 2682-2687 (2018)
The Scripps Research Institute
Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma.EBI
Bioorg Med Chem Lett 28: 2675-2678 (2018)
California Institute For Biomedical Research
Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation.EBI
Eur J Med Chem 152: 298-306 (2018)
Fudan University
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.EBI
Eur J Med Chem 152: 264-273 (2018)
Hebei University
Discovery of new erbB4 inhibitors: Repositioning an orphan chemical library by inverse virtual screening.EBI
Eur J Med Chem 152: 253-263 (2018)
University of Salerno
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.EBI
Bioorg Med Chem Lett 28: 2039-2049 (2018)
Jagiellonian University Medical College
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.EBI
Bioorg Med Chem 26: 3117-3125 (2018)
East China University of Science and Technology
Novel 8-hydroxyquinoline derivatives targeting ?-amyloid aggregation, metal chelation and oxidative stress against Alzheimer's disease.EBI
Bioorg Med Chem 26: 3191-3201 (2018)
Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.EBI
J Med Chem 61: 5162-5186 (2018)
University of Michigan
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.EBI
J Med Chem 61: 5034-5046 (2018)
University of Pennsylvania
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.EBI
J Med Chem 61: 4456-4475 (2018)
Ptc Therapeutics
Development of Thioaryl-Based Matrix Metalloproteinase-12 Inhibitors with Alternative Zinc-Binding Groups: Synthesis, Potentiometric, NMR, and Crystallographic Studies.EBI
J Med Chem 61: 4421-4435 (2018)
Universit£
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.EBI
Bioorg Med Chem Lett 28: 2055-2060 (2018)
Mitsubishi Tanabe Pharma
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.EBI
Eur J Med Chem 152: 235-252 (2018)
Peking University
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HEBI
Eur J Med Chem 152: 223-234 (2018)
Jagiellonian University Medical College
Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders.EBI
J Med Chem 61: 4436-4455 (2018)
Universit£
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.EBI
J Med Chem 61: 4635-4640 (2018)
Pfizer
Emerging Approaches for the Identification of Protein Targets of Small Molecules - A Practitioners' Perspective.EBI
J Med Chem 61: 8504-8535 (2018)
Abbvie
Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program.EBI
Bioorg Med Chem Lett 28: 2068-2073 (2018)
Pfizer
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.EBI
J Med Chem 61: 4608-4627 (2018)
China Pharmaceutical University
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.EBI
J Med Chem 61: 6964-6982 (2018)
Cadila Healthcare
NAD(P)H:Quinone Oxidoreductase 1 (NQO1) as a Therapeutic and Diagnostic Target in Cancer.EBI
J Med Chem 61: 6983-7003 (2018)
China Pharmaceutical University
Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy.EBI
Eur J Med Chem 152: 208-222 (2018)
Csir-Central Drug Research Institute
2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists.EBI
Bioorg Med Chem Lett 28: 2080-2083 (2018)
Sookmyung Women'S University
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaEBI
Bioorg Med Chem Lett 28: 2103-2108 (2018)
Amgen
Positive Modulators of the N-Methyl-d-aspartate Receptor: Structure-Activity Relationship Study of Steroidal 3-Hemiesters.EBI
J Med Chem 61: 4505-4516 (2018)
Institute of Physiology of The Czech Academy of Sciences
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.EBI
Bioorg Med Chem 26: 3773-3784 (2018)
Jagiellonian University Medical College
Screening serine/threonine and tyrosine kinase inhibitors for histidine kinase inhibition.EBI
Bioorg Med Chem 26: 5322-5326 (2018)
Indiana University
Synthesis, antimycobacterial activity and influence on mycobacterial InhA and PknB of 12-membered cyclodepsipeptides.EBI
Bioorg Med Chem 26: 3166-3190 (2018)
Martin-Luther-Universit£T Halle-Wittenberg
Structure-activity relationship of clovamide and its related compounds for the inhibition of amyloid? aggregation.EBI
Bioorg Med Chem 26: 3202-3209 (2018)
University of Tsukuba
Structure-based design of Trifarotene (CD5789), a potent and selective RAR? agonist for the treatment of acne.EBI
Bioorg Med Chem Lett 28: 1736-1741 (2018)
Nestle Skin Health
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.EBI
Bioorg Med Chem Lett 28: 1731-1735 (2018)
Nanjing University of Technology
Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker.EBI
Eur J Med Chem 152: 175-194 (2018)
Chinese Academy of Sciences
Design, synthesis, structure-activity relationships and X-ray structural studies of novel 1-oxopyrimido[4,5-c]quinoline-2-acetic acid derivatives as selective and potent inhibitors of human aldose reductase.EBI
Eur J Med Chem 152: 160-174 (2018)
Universitat Aut£Noma De Barcelona
Structure-activity relationship investigation of Phe-Arg mimetic region of human glutaminyl cyclase inhibitors.EBI
Bioorg Med Chem 26: 3133-3144 (2018)
Seoul National University
Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors.EBI
Bioorg Med Chem 26: 3217-3226 (2018)
Lanzhou University
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.EBI
Bioorg Med Chem Lett 28: 1679-1685 (2018)
Vanderbilt University
Kr÷hnke pyridines: Rapid and facile access to Mcl-1 inhibitors.EBI
Bioorg Med Chem Lett 28: 1949-1953 (2018)
University of Maryland
Identification of novel ?-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents.EBI
Eur J Med Chem 152: 148-159 (2018)
Csir-Central Drug Research Institute
Substituted 1,5-naphthyridine derivatives as novel antileishmanial agents. Synthesis and biological evaluation.EBI
Eur J Med Chem 152: 137-147 (2018)
Universidad De Le£N
Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines.EBI
Eur J Med Chem 152: 101-114 (2018)
University of Southampton
Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform.EBI
J Med Chem 61: 4335-4347 (2018)
University of Helsinki
Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor ? and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.EBI
J Med Chem 61: 4228-4248 (2018)
Duquesne University
Ligand Desolvation Steers On-Rate and Impacts Drug Residence Time of Heat Shock Protein 90 (Hsp90) Inhibitors.EBI
J Med Chem 61: 4397-4411 (2018)
University of Vienna
Discovery of d-amino acid oxidase inhibitors based on virtual screening against the lid-open enzyme conformation.EBI
Bioorg Med Chem Lett 28: 1693-1698 (2018)
Hungarian Academy of Sciences
Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model.EBI
Bioorg Med Chem Lett 28: 1686-1692 (2018)
Wuxi Apptec (Shanghai)
Novel amidrazone derivatives: Design, synthesis and activity evaluation.EBI
Bioorg Med Chem 26: 3158-3165 (2018)
Anhui Medical University
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.EBI
Eur J Med Chem 152: 76-86 (2018)
Chinese Academy of Sciences
Structure-Guided Design, Synthesis, and Characterization of Next-Generation Meprin ? Inhibitors.EBI
J Med Chem 61: 4578-4592 (2018)
Fraunhofer Institute For Cell Therapy and Immunology Izi
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.EBI
J Med Chem 61: 4176-4188 (2018)
TBA
The Notch Inhibitors Isolated from Nerium indicum.EBI
J Nat Prod 81: 1235-1240 (2018)
Chiba University
Inhibitors of dihydrofolate reductase as antitumor agents: design, synthesis and biological evaluation of a series of novel nonclassical 6-substituted pyrido[3,2-d]pyrimidines with a three- to five-carbon bridge.EBI
Bioorg Med Chem 26: 2674-2685 (2018)
Perking University
Targeting species specific amino acid residues: Design, synthesis and biological evaluation of 6-substituted pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors and potential anti-opportunistic infection agents.EBI
Bioorg Med Chem 26: 2640-2650 (2018)
Duquesne University
Development of piperazine-based hydroxamic acid inhibitors against falcilysin, an essential malarial protease.EBI
Bioorg Med Chem Lett 28: 1846-1848 (2018)
California State University
Targeting lysine specific demethylase 4A (KDM4A) tandem TUDOR domain - A fragment based approach.EBI
Bioorg Med Chem Lett 28: 1708-1713 (2018)
Abbvie
Identification of novel 2-benzyl-1-indanone analogs as interleukin-5 inhibitors.EBI
Eur J Med Chem 152: 65-75 (2018)
Chungnam National University
Discovery of N-{3-[(ethanimidoylamino)methyl]benzyl}-l-prolinamide dihydrochloride: A new potent and selective inhibitor of the inducible nitric oxide synthase as a promising agent for the therapy of malignant glioma.EBI
Eur J Med Chem 152: 53-64 (2018)
University of Chieti "G. D'Annunzio
Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor.EBI
J Med Chem 61: 4370-4385 (2018)
Rti International
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.EBI
J Med Chem 61: 4386-4396 (2018)
Agency For Science, Technology and Research (A*Star)
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.EBI
Bioorg Med Chem 26: 2514-2529 (2018)
Marquette University
Synthesis, structure and bioactivity of primary sulfamate-containing natural products.EBI
Bioorg Med Chem Lett 28: 3009-3013 (2018)
Griffith University
Design, synthesis and biological evaluation of novel xanthine oxidase inhibitors bearing a 2-arylbenzo[b]furan scaffold.EBI
Eur J Med Chem 151: 849-860 (2018)
China Pharmaceutical University
Synthesis and biological evaluation of 2,6-disubstituted-9H-purine, 2,4-disubstitued-thieno[3,2-d]pyrimidine and -7H-pyrrolo[2,3-d]pyrimidine analogues as novel CHK1 inhibitors.EBI
Eur J Med Chem 151: 836-848 (2018)
Peking University
Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform.EBI
Eur J Med Chem 152: 1-9 (2018)
Egyptian Russian University
Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.EBI
J Med Chem 61: 4348-4369 (2018)
Agency For Science, Technology and Research (A*Star)
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).EBI
J Med Chem 61: 3823-3841 (2018)
Astrazeneca
Novel naphthyloxy derivatives - Potent histamine HEBI
Bioorg Med Chem 26: 2573-2585 (2018)
Jagiellonian University Medical College
Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B.EBI
Bioorg Med Chem 26: 2621-2631 (2018)
Shenyang Pharmaceutical University
Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia.EBI
Bioorg Med Chem Lett 28: 1725-1730 (2018)
Taisho Pharmaceutical
Fluorescent-Labeled Selective Adenosine AEBI
J Med Chem 61: 4301-4316 (2018)
University of Bonn
Highly Selective and Potent Ectonucleotide Pyrophosphatase-1 (NPP1) Inhibitors Based on Uridine 5'-PEBI
J Med Chem 61: 3939-3951 (2018)
Bar-Ilan University
Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NHEBI
Eur J Med Chem 151: 815-823 (2018)
University of Arizona
Structural insights into serotonin receptor ligands polypharmacology.EBI
Eur J Med Chem 151: 797-814 (2018)
Polish Academy of Sciences
Design, synthesis, molecular modelling and in vitro cytotoxicity analysis of novel carbamate derivatives as inhibitors of Monoacylglycerol lipase.EBI
Bioorg Med Chem 26: 2561-2572 (2018)
Universit£
Preliminary in vitro and in vivo investigation of a potent platelet derived growth factor receptor (PDGFR) family kinase inhibitor.EBI
Bioorg Med Chem Lett 28: 1781-1784 (2018)
University of The Pacific
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.EBI
Bioorg Med Chem Lett 28: 1804-1810 (2018)
Abbvie
Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2).EBI
Eur J Med Chem 151: 777-796 (2018)
Sun Yat-Sen University
Identification of Lycopodium Alkaloids Produced by an Ultraviolet-Irradiated Strain of Paraboeremia, an Endophytic Fungus from Lycopodium serratum var. longipetiolatum.EBI
J Nat Prod 81: 1143-1147 (2018)
Nagoya City University
Harnessing pyrrolidine iminosugars into dimeric structures for the rapid discovery of divalent glycosidase inhibitors.EBI
Eur J Med Chem 151: 765-776 (2018)
University of Seville
Novel fatty acid chain modified GLP-1 derivatives with prolonged in vivo glucose-lowering ability and balanced glucoregulatory activity.EBI
Bioorg Med Chem 26: 2599-2609 (2018)
China Pharmaceutical University
Optimized allosteric inhibition of engineered protein tyrosine phosphatases with an expanded palette of biarsenical small molecules.EBI
Bioorg Med Chem 26: 2610-2620 (2018)
Amherst College
Discovery and evaluation of nNaEBI
Bioorg Med Chem 26: 2428-2436 (2018)
University of Alabama At Birmingham
Discovery of NEBI
J Med Chem 61: 3855-3869 (2018)
Palack£
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.EBI
J Med Chem 61: 3870-3888 (2018)
Vrije Universiteit Amsterdam
Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.EBI
J Med Chem 62: 247-265 (2019)
Pfizer
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.EBI
J Nat Prod 81: 1029-1035 (2018)
Indiana State University
Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.EBI
ACS Med Chem Lett 9: 392-396 (2018)
Novartis Institutes For Biomedical Research
Conformationally Constrained Cinnolinone Nucleoside Analogues as Siderophore Biosynthesis Inhibitors for Tuberculosis.EBI
ACS Med Chem Lett 9: 386-391 (2018)
University of Minnesota
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.EBI
ACS Med Chem Lett 9: 370-375 (2018)
Shandong University
Discovery of EBI
ACS Med Chem Lett 9: 354-358 (2018)
Cytokinetics
A BODIPY-Tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase.EBI
ACS Med Chem Lett 9: 345-350 (2018)
University of Bonn
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.EBI
ACS Med Chem Lett 9: 334-338 (2018)
Shandong University
Manumycin A Is a Potent Inhibitor of Mammalian Thioredoxin Reductase-1 (TrxR-1).EBI
ACS Med Chem Lett 9: 318-322 (2018)
Florida International University
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.EBI
ACS Med Chem Lett 9: 312-317 (2018)
East China University of Science and Technology
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.EBI
ACS Med Chem Lett 9: 300-305 (2018)
Agios Pharmaceuticals
Toll-like Receptors for the Treatment of Autoimmune, Inflammation, and Infectious Diseases.EBI
ACS Med Chem Lett 9: 296-297 (2018)
Usona Institute
Therapeutic Potential of FXR Agonists in the Treatment of Multiple Diseases.EBI
ACS Med Chem Lett 9: 294-295 (2018)
Therachem Research Medilab
ATR Inhibitors as Potential Treatment for Cancers.EBI
ACS Med Chem Lett 9: 292-293 (2018)
Therachem Research Medilab
Azabicyclic Fused Pyrimidine Derivatives Useful for the Treatment of Alzheimer's Disease.EBI
ACS Med Chem Lett 9: 290-291 (2018)
Temple University
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents.EBI
Bioorg Med Chem 26: 2452-2465 (2018)
Takeda Pharmaceutical
Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over ?-Arrestin 2 Recruitment) Within the Melanocortin Receptors.EBI
J Med Chem 62: 144-158 (2019)
University of Minnesota
Structure-Based Design of Inhibitors Targeting PrfA, the Master Virulence Regulator of Listeria monocytogenes.EBI
J Med Chem 61: 4165-4175 (2018)
TBA
Antibacterial Dimeric Acylphloroglucinols from Hypericum japonicum.EBI
J Nat Prod 81: 1098-1102 (2018)
Chinese Academy of Sciences
Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening.EBI
Eur J Med Chem 151: 740-751 (2018)
Shanghai University
NEBI
J Med Chem 61: 4528-4560 (2018)
Helmholtz-Zentrum Dresden-Rossendorf
Rational design and screening of peptide-based inhibitors of heat shock factor 1 (HSF1).EBI
Bioorg Med Chem 26: 5299-5306 (2018)
University of California At San Francisco
Design, synthesis, and evaluation of novel N-1 fluoroquinolone derivatives: Probing for binding contact with the active site tyrosine of gyrase.EBI
Bioorg Med Chem Lett 28: 1903-1910 (2018)
University of Iowa
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).EBI
J Med Chem 61: 4249-4255 (2018)
Harvard Medical School
Development of Macrocyclic Peptidomimetics Containing Constrained ?,?-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.EBI
J Med Chem 61: 4263-4269 (2018)
University of Naples "Federico Ii
Agonists of the ?-aminobutyric acid type B (GABAEBI
Bioorg Med Chem Lett 28: 2697-2700 (2018)
University of Mississippi
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.EBI
Bioorg Med Chem Lett 28: 1811-1816 (2018)
Celgene Quanticel Research
Substituent effect of N-benzylated gramine derivatives that prevent the PP2A inhibition and dissipate the neuronal CaEBI
Bioorg Med Chem 26: 2551-2560 (2018)
Universidad Aut£Noma De Madrid
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.EBI
J Med Chem 61: 4317-4334 (2018)
University of Strathclyde
An overview of quinazolines: Pharmacological significance and recent developments.EBI
NA
Mnr College of Pharmacy
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
Eur J Med Chem 151: 557-567 (2018)
University of Texas At Austin
Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition.EBI
Eur J Med Chem 151: 533-545 (2018)
National Health Research Institutes
Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes.EBI
Bioorg Med Chem Lett 28: 1849-1852 (2018)
Cadila Healthcare
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.EBI
Bioorg Med Chem Lett 28: 1887-1891 (2018)
Eli Lilly
Practical application of ligand efficiency metrics in lead optimisation.EBI
Bioorg Med Chem 26: 3006-3015 (2018)
Astrazeneca
Structure activity relationship studies on rhodanines and derived enethiol inhibitors of metallo-?-lactamases.EBI
Bioorg Med Chem 26: 2928-2936 (2018)
University of Oxford
Discovery of novel Methylsulfonyl phenyl derivatives as potent human Cyclooxygenase-2 inhibitors with effective anticonvulsant action: Design, synthesis, in-silico, in-vitro and in-vivo evaluation.EBI
Eur J Med Chem 151: 520-532 (2018)
University of Delhi
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.EBI
Bioorg Med Chem Lett 28: 1958-1963 (2018)
Glaxosmithkline
MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.EBI
Bioorg Med Chem Lett 28: 1954-1957 (2018)
Merck
Highlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530).EBI
J Med Chem 61: 4052-4066 (2018)
Abbvie
Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand.EBI
J Med Chem 61: 4020-4029 (2018)
University of Shizuoka
Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example.EBI
J Med Chem 61: 7448-7470 (2018)
Monash University
A new class of pyrazolo[5,1-c][1,2,4]triazines as ?-aminobutyric type A (GABAEBI
Bioorg Med Chem 26: 2475-2487 (2018)
Universit£
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.EBI
Bioorg Med Chem 26: 2992-2995 (2018)
University of Dundee
Quinone skeleton as a new class of irreversible inhibitors against Staphylococcus aureus sortase A.EBI
Bioorg Med Chem Lett 28: 1864-1869 (2018)
Shanghai Institute of Materia Medica
P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor.EBI
Bioorg Med Chem Lett 28: 1853-1859 (2018)
Bristol-Myers Squibb Research and Development
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.EBI
Bioorg Med Chem Lett 28: 1972-1980 (2018)
University of Michigan
Structure-activity relationship study of a series of caspase inhibitors containing ?-amino acid moiety for treatment of cholestatic liver disease.EBI
Bioorg Med Chem Lett 28: 1874-1878 (2018)
Wuxi Apptec (Shanghai)
Synthesis of 7?-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors.EBI
Eur J Med Chem 151: 495-507 (2018)
University of Helsinki
Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.EBI
Eur J Med Chem 151: 462-481 (2018)
Gwangju Institute of Science and Technology (Gist)
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.EBI
Eur J Med Chem 151: 450-461 (2018)
University of Texas Medical Branch
Discovery of N-hydroxy-3-alkoxybenzamides as direct acid sphingomyelinase inhibitors using a ligand-based pharmacophore model.EBI
Eur J Med Chem 151: 389-400 (2018)
China Pharmaceutical University
Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.EBI
J Med Chem 61: 4030-4051 (2018)
Nestl�
Tight-Binding Inhibition of Human Monoamine Oxidase B by Chromone Analogs: A Kinetic, Crystallographic, and Biological Analysis.EBI
J Med Chem 61: 4203-4212 (2018)
University of Porto
Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGF?) Production in Regulatory T-Cells.EBI
J Med Chem 61: 4135-4154 (2018)
Nce Discovery (Domainex)
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ER? Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.EBI
J Nat Prod 81: 966-975 (2018)
TBA
Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.EBI
J Med Chem 61: 4155-4164 (2018)
Nankai University
2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.EBI
Bioorg Med Chem 26: 2488-2500 (2018)
Latvian Institute of Organic Synthesis
Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKC? phosphorylation: Potential therapy to modulate T cell dependent immunity.EBI
Bioorg Med Chem Lett 28: 1964-1971 (2018)
Biogen
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EPEBI
Bioorg Med Chem Lett 28: 1892-1896 (2018)
Glaxosmithkline
2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and inávivo activity for a new class of intraocular pressure lowering agents.EBI
Eur J Med Chem 151: 363-375 (2018)
University of Florence
Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.EBI
Eur J Med Chem 151: 351-362 (2018)
Shenyang Pharmaceutical University
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.EBI
Eur J Med Chem 151: 339-350 (2018)
Shandong University
Targeting Tyrosinase: Development and Structural Insights of Novel Inhibitors Bearing Arylpiperidine and Arylpiperazine Fragments.EBI
J Med Chem 61: 3908-3917 (2018)
Universit�
Drimane Sesquiterpenoids Noncompetitively Inhibit Human ?4?2 Nicotinic Acetylcholine Receptors with Higher Potency Compared to Human ?3?4 and ?7 Subtypes.EBI
J Nat Prod 81: 811-817 (2018)
California Northstate University College of Medicine
Structural Modification of Natural Product Ganomycin I Leading to Discovery of a ?-Glucosidase and HMG-CoA Reductase Dual Inhibitor Improving Obesity and Metabolic Dysfunction in Vivo.EBI
J Med Chem 61: 3609-3625 (2018)
University of Chinese Academy of Sciences
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI
Bioorg Med Chem Lett 28: 1446-1455 (2018)
Phenex Pharmaceuticals
Callyspongiamides A and B, sterol O-acyltransferase inhibitors, from the Indonesian marine sponge Callyspongia sp.EBI
Bioorg Med Chem Lett 28: 1911-1914 (2018)
Tohoku Medical and Pharmaceutical University
The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation.EBI
Bioorg Med Chem Lett 28: 1550-1557 (2018)
Bristol-Myers Squibb Research and Development
Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine DEBI
Bioorg Med Chem Lett 28: 1897-1902 (2018)
Southern Illinois University Edwardsville
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-RafEBI
Bioorg Med Chem 26: 2381-2391 (2018)
Yantai University
Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors.EBI
Bioorg Med Chem 26: 2410-2419 (2018)
Astellas Pharma
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.EBI
Eur J Med Chem 151: 315-326 (2018)
Shaanxi University of Science & Technology
Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) ?/?.EBI
J Med Chem 61: 4087-4102 (2018)
Ulm University Hospital
Design of Aminopeptidase N Inhibitors as Anti-cancer Agents.EBI
J Med Chem 61: 6468-6490 (2018)
Jadavpur University
Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPAR? selective agonists: New leads for oculovascular conditions.EBI
Bioorg Med Chem Lett 28: 2717-2722 (2018)
University of Oklahoma
Reversible, orally available ADP receptor (P2YEBI
Bioorg Med Chem Lett 28: 1459-1463 (2018)
King Abdullah International Medical Research Center/King Saud Bin Abdulaziz University For Health Sciences
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations.EBI
Bioorg Med Chem Lett 28: 1476-1483 (2018)
University of Jinan
Novel thioureido-benzenesulfonamide derivatives with enaminone linker as potent anticancer, radiosensitizers and VEGFR2 inhibitors.EBI
Bioorg Med Chem Lett 28: 1464-1470 (2018)
National Center For Radiation Research and Technology (Ncrrt)
Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.EBI
J Med Chem 61: 3685-3696 (2018)
Pfizer
Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).EBI
Eur J Med Chem 151: 304-314 (2018)
Icahn School of Medicine At Mount Sinai
Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.EBI
Bioorg Med Chem Lett 28: 1507-1515 (2018)
University of Michigan
Structure-based design and discovery of potent and selective KDM5 inhibitors.EBI
Bioorg Med Chem Lett 28: 1490-1494 (2018)
Celgene
Development of novel pyridazinone-based adenosine receptor ligands.EBI
Bioorg Med Chem Lett 28: 1484-1489 (2018)
Universit£
Synthesis and biological evaluation of clovamide analogues as potent anti-neuroinflammatory agents inávitro and inávivo.EBI
Eur J Med Chem 151: 261-271 (2018)
China Pharmaceutical University
Phthalimide conjugations for the degradation of oncogenic PI3K.EBI
Eur J Med Chem 151: 237-247 (2018)
Tsinghua University
Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels.EBI
Bioorg Med Chem 26: 3046-3059 (2018)
Iitb-Monash Research Academy
Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HTEBI
J Med Chem 62: 288-305 (2019)
TBA
Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.EBI
J Med Chem 61: 3697-3711 (2018)
National and Kapodistrian University of Athens
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.EBI
J Med Chem 61: 6421-6467 (2018)
Glaxosmithkline
Toward?-Secretase-1 Inhibitors with Improved Isoform Selectivity.EBI
J Med Chem 61: 3491-3502 (2018)
Astrazeneca
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).EBI
J Med Chem 61: 4704-4719 (2018)
Athenex
Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-?/FFAR1 agonists.EBI
Bioorg Med Chem Lett 28: 1595-1602 (2018)
Suez Canal University
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.EBI
Bioorg Med Chem Lett 28: 1540-1544 (2018)
Irbm Science Park
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives.EBI
Bioorg Med Chem Lett 28: 1534-1539 (2018)
Luoyang Normal University
A review of salvinorin analogs and their kappa-opioid receptor activity.EBI
NA
The Scripps Research Institute
New potent and selective AEBI
Eur J Med Chem 151: 199-213 (2018)
University of Camerino
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.EBI
J Med Chem 61: 3541-3550 (2018)
University of California Davis
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.EBI
J Med Chem 61: 4476-4504 (2018)
Pfizer
Discovery of a quinoline-based phenyl sulfone derivative as an antitrypanosomal agent.EBI
Bioorg Med Chem Lett 28: 1647-1651 (2018)
Jackson State University
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.EBI
Eur J Med Chem 151: 145-157 (2018)
Chinese Academy of Sciences
Benzopyrroloxazines containing a bridgehead nitrogen atom as promising scaffolds for the achievement of biologically active agents.EBI
Eur J Med Chem 151: 121-144 (2018)
University of Calabria
Structure-Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3).EBI
J Med Chem 61: 3745-3751 (2018)
Kyoto University
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.EBI
J Med Chem 61: 3674-3684 (2018)
The University of Queensland
Success stories of natural product-based hybrid molecules for multi-factorial diseases.EBI
Eur J Med Chem 151: 62-97 (2018)
Punjabi University
Designing novel inhibitors against falcipain-2 of Plasmodium falciparum.EBI
Bioorg Med Chem Lett 28: 1566-1569 (2018)
Delhi Institute of Pharmaceutical Sciences and Research
Structure-activity relationships in a new class of non-substrate-like covalent inhibitors of the bacterial glycosyltransferase LgtC.EBI
Bioorg Med Chem 26: 2973-2983 (2018)
King'S College London
DNA sequence-specific ligands. XVII. Synthesis, spectral properties, virological and biochemical studies of fluorescent dimeric bisbenzimidazoles DBA(n).EBI
Bioorg Med Chem 26: 2302-2309 (2018)
Engelhardt Institute of Molecular Biology Russian Academy of Sciences
Design, synthesis, and biological evaluation of new B-RafEBI
Bioorg Med Chem 26: 2372-2380 (2018)
Nanjing University
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.EBI
Bioorg Med Chem 26: 3039-3045 (2018)
Imperial College
Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid.EBI
Eur J Med Chem 150: 930-945 (2018)
University of Torino
Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.EBI
Eur J Med Chem 150: 809-816 (2018)
China Pharmaceutical University
Discovery of novel quinazolinone derivatives as high potent and selective PI3K? and PI3K?/? inhibitors.EBI
Eur J Med Chem 151: 9-17 (2018)
Shandong University
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.EBI
J Med Chem 61: 3626-3640 (2018)
Pfizer
Site-specific effect of polar functional group-modification in lipids of TLR2 ligands for modulating the ligand immunostimulatory activity.EBI
Bioorg Med Chem Lett 28: 1638-1641 (2018)
Keio University
Identification of multi-target inhibitors of leukotriene and prostaglandin EEBI
Eur J Med Chem 150: 876-899 (2018)
Gazi University
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.EBI
J Med Chem 61: 3565-3581 (2018)
Sanofi R&D
Tetrahydroquinoline Ring as a Versatile Bioisostere of Tetralin for Melatonin Receptor Ligands.EBI
J Med Chem 61: 3726-3737 (2018)
Universit£
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.EBI
J Med Chem 61: 3370-3388 (2018)
Eth Zurich
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.EBI
J Med Chem 61: 3350-3369 (2018)
Eth Zurich
Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.EBI
J Med Chem 61: 3641-3659 (2018)
Pharmaron-Beijing
Lipophilic Efficiency as an Important Metric in Drug Design.EBI
J Med Chem 61: 6401-6420 (2018)
Pfizer
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DEBI
J Med Chem 61: 3712-3725 (2018)
Universit£
Nanomolar-Potency 1,2,4-Triazoloquinoxaline Inhibitors of the Kidney Urea Transporter UT-A1.EBI
J Med Chem 61: 3209-3217 (2018)
San Francisco State University
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.EBI
J Med Chem 61: 3454-3477 (2018)
University of Regensburg
Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.EBI
Bioorg Med Chem Lett 28: 1615-1620 (2018)
Gsk Pharmaceuticals R&D
Design and Synthesis of Novel Positive Allosteric Modulators of ?7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.EBI
J Med Chem 62: 159-173 (2019)
Peking University
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ER?/VEGFR-2 ligands with anti-breast cancer activity.EBI
Eur J Med Chem 150: 783-795 (2018)
China Pharmaceutical University
Bicyclic Helical Peptides as Dual Inhibitors Selective for Bcl2A1 and Mcl-1 Proteins.EBI
J Med Chem 61: 2962-2972 (2018)
The University of Queensland
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.EBI
J Med Chem 61: 2949-2961 (2018)
Sungkyunkwan University
Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins.EBI
J Med Chem 61: 3660-3673 (2018)
Max Planck Institute of Psychiatry
Human?-Defensiná1 and?-Defensiná3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.EBI
J Med Chem 61: 3738-3744 (2018)
University of Florida
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.EBI
J Nat Prod 81: 998-1006 (2018)
Yunnan University
Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors.EBI
Bioorg Med Chem 26: 2173-2185 (2018)
Xi'An Jiaotong University
2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships.EBI
Bioorg Med Chem 26: 2107-2150 (2018)
Glaxosmithkline Research and Development
Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors.EBI
Bioorg Med Chem 26: 2186-2197 (2018)
Chinese Academy of Medical Sciences & Peking Union Medical College
Design and synthesis of aryloxypropanolamine as ?EBI
Eur J Med Chem 150: 757-770 (2018)
East China Normal University
Inhibitors of phosphodiesterase as cancer therapeutics.EBI
Eur J Med Chem 150: 742-756 (2018)
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Structure-based design of bacterial transglycosylase inhibitors incorporating biphenyl, amine linker and 2-alkoxy-3-phosphorylpropanoate moieties.EBI
Eur J Med Chem 150: 729-741 (2018)
National Taiwan University
Sulfoximines as potent ROR? inverse agonists.EBI
Bioorg Med Chem Lett 28: 1269-1273 (2018)
Nestle Skin Health
Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.EBI
Eur J Med Chem 150: 698-718 (2018)
University of Siena
Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors.EBI
Eur J Med Chem 150: 678-686 (2018)
Kurukshetra University
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.EBI
J Med Chem 61: 3114-3125 (2018)
Pfizer
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.EBI
Eur J Med Chem 150: 667-677 (2018)
Taipei Medical University
Synthesis and antikinetoplastid evaluation of bis(benzyl)spermidine derivatives.EBI
Eur J Med Chem 150: 655-666 (2018)
Universit£
Evaluation of analogues of furan-amidines as inhibitors of NQO2.EBI
Bioorg Med Chem Lett 28: 1292-1297 (2018)
University of Manchester
Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.EBI
Bioorg Med Chem 26: 2965-2972 (2018)
University of Oxford
Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors.EBI
Bioorg Med Chem 26: 2165-2172 (2018)
Shanghai Institute of Pharmaceutical Industry
Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).EBI
J Med Chem 61: 3037-3058 (2018)
Guangzhou Medical University
Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation.EBI
J Med Chem 61: 3151-3165 (2018)
University of Delhi
Structure-Based Optimization of Small-Molecule Inhibitors for the ?-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.EBI
J Med Chem 61: 2989-3007 (2018)
H. Lee Moffitt Cancer Center and Research Institute
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.EBI
J Med Chem 61: 2837-2864 (2018)
Novartis Institutes For Biomedical Research
Small-Molecule Activator of UNC-51-Like Kinase 1 (ULK1) That Induces Cytoprotective Autophagy for Parkinson's Disease Treatment.EBI
J Med Chem 61: 2776-2792 (2018)
Sichuan University
4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors.EBI
J Med Chem 61: 3076-3088 (2018)
TBA
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.EBI
Bioorg Med Chem Lett 28: 1336-1341 (2018)
Astrazeneca
New phenylaniline derivatives as modulators of amyloid protein precursor metabolism.EBI
Bioorg Med Chem 26: 2151-2164 (2018)
University of Lille
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.EBI
Bioorg Med Chem 26: 2051-2060 (2018)
Shandong University
Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2YEBI
J Med Chem 61: 3089-3113 (2018)
University Park Nottingham
Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61.EBI
J Nat Prod 81: 949-956 (2018)
Zhejiang University
A genetically selected cyclic peptide inhibitor of BCL6 homodimerization.EBI
Bioorg Med Chem 26: 3034-3038 (2018)
University of Southampton
Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.EBI
Bioorg Med Chem 26: 1727-1739 (2018)
National Center For Advancing Translational Sciences
Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HTEBI
Bioorg Med Chem Lett 28: 1381-1385 (2018)
University of Houston
Antibacterial Muraymycins from Mutant Strains of Streptomyces sp. NRRL 30471.EBI
J Nat Prod 81: 942-948 (2018)
Nanjing University of Chinese Medicine
Structure-based drug design of 1,3,6-trisubstituted 1,4-diazepan-7-ones as selective human kallikrein 7 inhibitors.EBI
Bioorg Med Chem Lett 28: 1371-1375 (2018)
Asubio Pharma
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.EBI
Bioorg Med Chem Lett 28: 1386-1391 (2018)
Chinese Academy of Medical Sciences and Peking Union Medical College
Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities.EBI
Eur J Med Chem 150: 567-578 (2018)
Beni-Suef University
Drug discovery in tuberculosis. New drug targets and antimycobacterial agents.EBI
NA
Universidade De Lisboa
Design, synthesis, biological evaluation and inávivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.EBI
Eur J Med Chem 150: 506-524 (2018)
University of Navarra
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.EBI
Eur J Med Chem 150: 491-505 (2018)
Universit£
Identification of second-generation P2X3 antagonists for treatment of pain.EBI
Bioorg Med Chem Lett 28: 1392-1396 (2018)
Merck
Design, synthesis, and evaluation of simple phenol amides as ERR? agonists.EBI
Bioorg Med Chem Lett 28: 1313-1319 (2018)
The Scripps Research Institute
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.EBI
Eur J Med Chem 150: 446-456 (2018)
Universit£
Novel ciprofloxacin hybrids using biology oriented drug synthesis (BIODS) approach: Anticancer activity, effects on cell cycle profile, caspase-3 mediated apoptosis, topoisomerase II inhibition, and antibacterial activity.EBI
Eur J Med Chem 150: 403-418 (2018)
Cairo University
Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.EBI
J Med Chem 61: 2680-2693 (2018)
St. Jude Children'S Research Hospital
Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.EBI
J Med Chem 61: 2694-2706 (2018)
St. Jude Children'S Research Hospital
New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold.EBI
J Med Chem 61: 3389-3408 (2018)
University of Bonn
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).EBI
Bioorg Med Chem Lett 28: 1357-1362 (2018)
National University of Singapore
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI
Bioorg Med Chem Lett 28: 1397-1403 (2018)
Merck
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.EBI
Bioorg Med Chem Lett 28: 1188-1193 (2018)
South China Agricultural University
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFR? kinase inhibitor for PDGFR? driving chronic eosinophilic leukemia.EBI
Eur J Med Chem 150: 366-384 (2018)
Chinese Academy of Sciences
Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element.EBI
Eur J Med Chem 150: 334-346 (2018)
Wichita State University
Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the MEBI
J Med Chem 61: 2875-2894 (2018)
Monash University (Parkville Campus)
Discovery of Nanomolar Desmuramylpeptide Agonists of the Innate Immune Receptor Nucleotide-Binding Oligomerization Domain-Containing Protein 2 (NOD2) Possessing Immunostimulatory Properties.EBI
J Med Chem 61: 2707-2724 (2018)
University of Ljubljana
Analyses of Synthetic N-Acyl Dopamine Derivatives Revealing Different Structural Requirements for Their Anti-inflammatory and Transient-Receptor-Potential-Channel-of-the-Vanilloid-Receptor-Subfamily-Subtype-1 (TRPV1)-Activating Properties.EBI
J Med Chem 61: 3126-3137 (2018)
Mannheim University of Applied Sciences
Stereochemical Structure Activity Relationship Studies (S-SAR) of Tetrahydrolipstatin.EBI
ACS Med Chem Lett 9: 274-278 (2018)
Northeastern University
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.EBI
ACS Med Chem Lett 9: 268-273 (2018)
Duke University Medical Center
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.EBI
ACS Med Chem Lett 9: 262-267 (2018)
Guangzhou Medical University
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.EBI
ACS Med Chem Lett 9: 256-261 (2018)
Wuxi Apptec (Shanghai) Co.
Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.EBI
ACS Med Chem Lett 9: 250-255 (2018)
University of Hawaii Cancer Center
Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors.EBI
ACS Med Chem Lett 9: 238-243 (2018)
Almac Discovery
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant EBI
ACS Med Chem Lett 9: 233-237 (2018)
East China University of Science and Technology
In Search of the Optimal Macrocyclization Site for Neurotensin.EBI
ACS Med Chem Lett 9: 227-232 (2018)
Universit£
Mitigating the Metabolic Liability of Carbonyl Reduction: Novel Calpain Inhibitors with P1' Extension.EBI
ACS Med Chem Lett 9: 221-226 (2018)
Abbvie Deutschland
2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.EBI
ACS Med Chem Lett 9: 215-220 (2018)
Novartis Institutes For Biomedical Research
Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.EBI
ACS Med Chem Lett 9: 210-214 (2018)
Montclair State University
Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.EBI
ACS Med Chem Lett 9: 198-203 (2018)
National and Kapodistrian University of Athens
Dual GSK-3?/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.EBI
ACS Med Chem Lett 9: 171-176 (2018)
China Pharmaceutical University
Thiazole Derivatives as Inhibitors for the Treatment of Cancer Cells Resistant.EBI
ACS Med Chem Lett 9: 169-170 (2018)
Usona Institute
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.EBI
ACS Med Chem Lett 9: 167-168 (2018)
Usona Institute
Azabicyclic Fused Pyrimidine Derivatives Useful for the Treatment of Alzheimer's Disease.EBI
ACS Med Chem Lett 9: 165-166 (2018)
Temple University
Allosteric Modulators of Nicotinic Acetylcholine Receptors Useful for the Treatment of Cognitive Impairment.EBI
ACS Med Chem Lett 9: 163-164 (2018)
Temple University
Acyl Sulfonamides NaV1.7 Blockers Useful for the Treatment of Pain.EBI
ACS Med Chem Lett 9: 161-162 (2018)
Temple University
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.EBI
J Med Chem 61: 3193-3208 (2018)
The University of Texas M.D. Anderson Cancer Center
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3K?) inhibitors.EBI
Bioorg Med Chem 26: 2028-2040 (2018)
Xi'An Jiaotong University
Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay.EBI
Bioorg Med Chem 26: 1751-1758 (2018)
University of Science and Technology of China
Perfluoroarene-based peptide macrocycles that inhibit the Nrf2/Keap1 interaction.EBI
Bioorg Med Chem Lett 28: 2728-2731 (2018)
University of East Anglia
Identification of an aminothiazole series of ROR? modulators.EBI
Bioorg Med Chem Lett 28: 1178-1181 (2018)
The Scripps Research Institute
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.EBI
Bioorg Med Chem Lett 28: 1348-1351 (2018)
Shandong University
Discovery of N-aryl-N'-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors.EBI
Bioorg Med Chem Lett 28: 1257-1261 (2018)
Shanghai Haiyan Pharmaceutical Technology Co. Itd.
A novel templates of piperazinyl-1,2-dihydroquinoline-3-carboxylates: Synthesis, anti-microbial evaluation and molecular docking studies.EBI
Bioorg Med Chem Lett 28: 1166-1170 (2018)
Csir-Institute of Chemical Technology
Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.EBI
Bioorg Med Chem Lett 28: 1122-1126 (2018)
Merck
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.EBI
Eur J Med Chem 150: 292-306 (2018)
University of Defence
Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.EBI
Eur J Med Chem 150: 282-291 (2018)
Shandong University
Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation.EBI
Bioorg Med Chem 26: 1961-1970 (2018)
Fudan University
Synthesis and antimycobacterial activity of 1-(?-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.EBI
Eur J Med Chem 150: 268-281 (2018)
University of Delhi
Identification of small-molecule inhibitors of USP2a.EBI
Eur J Med Chem 150: 261-267 (2018)
Jagiellonian University
Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy?EBI
Eur J Med Chem 150: 206-227 (2018)
Instituto De Qu£Mica M£Dica (Iqm, Csic)
Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding.EBI
J Med Chem 61: 2793-2805 (2018)
Hauptman-Woodward Medical Research Institute
Design, Synthesis, and Biological Activity of New N-(Phenylmethyl)-benzoxazol-2-thiones as Macrophage Migration Inhibitory Factor (MIF) Antagonists: Efficacies in Experimental Pulmonary Hypertension.EBI
J Med Chem 61: 2725-2736 (2018)
Hospital Marie Lannelongue
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.EBI
J Med Chem 61: 3516-3540 (2018)
Effector Therapeutics
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.EBI
Eur J Med Chem 150: 156-175 (2018)
Chinese Academy of Sciences
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine AEBI
Eur J Med Chem 150: 127-139 (2018)
Universit£
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives.EBI
Bioorg Med Chem 26: 1986-1995 (2018)
Istanbul Medipol University
Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.EBI
Bioorg Med Chem 26: 1638-1642 (2018)
Nagasaki University
Identification of caffeoylquinic acid derivatives as natural protein tyrosine phosphatase 1B inhibitors from Artemisia princeps.EBI
Bioorg Med Chem Lett 28: 1194-1197 (2018)
China Pharmaceutical University
Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease.EBI
Eur J Med Chem 150: 87-101 (2018)
Banaras Hindu University
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.EBI
Bioorg Med Chem 26: 1896-1908 (2018)
Chinese Academy of Sciences
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Bioorg Med Chem 26: 1740-1750 (2018)
Beijing Normal University
Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.EBI
Bioorg Med Chem Lett 28: 1182-1187 (2018)
Janssen Research and Development
Ligand-Based NMR Study of C-X-C Chemokine Receptor Type 4 (CXCR4)-Ligand Interactions on Living Cancer Cells.EBI
J Med Chem 61: 2910-2923 (2018)
Universit£
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.EBI
J Med Chem 61: 9085-9104 (2018)
Chinese Academy of Sciences
Small molecule modulators of PCSK9 - A literature and patent overview.EBI
Bioorg Med Chem Lett 28: 1155-1160 (2018)
Astrazeneca
Alleviating CYP and hERG liabilities by structure optimization of dihydrofuran-fused tricyclic benzo[d]imidazole series - Potent, selective and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-2.EBI
Bioorg Med Chem Lett 28: 1211-1218 (2018)
Glenmark Pharmaceuticals
Inhibition of histone lysine methyltransferases G9a and GLP by ejection of structural Zn(II).EBI
Bioorg Med Chem Lett 28: 1234-1238 (2018)
Radboud University
Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure.EBI
Bioorg Med Chem Lett 28: 1228-1233 (2018)
Japan Tobacco
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.EBI
Bioorg Med Chem 26: 1920-1928 (2018)
Kindai University
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.EBI
J Med Chem 61: 3059-3075 (2018)
China Pharmaceutical University
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.EBI
J Med Chem 61: 3166-3192 (2018)
Nankai University
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI
J Med Chem 61: 2823-2836 (2018)
Bicycle Therapeutics
Catecholic Isoquinolines from Portulaca oleracea and Their Anti-inflammatory and ?EBI
J Nat Prod 81: 768-777 (2018)
Shandong University
A combination ofEBI
Bioorg Med Chem 26: 1929-1938 (2018)
The University of Tokyo
Discovery of Novel KRAS-PDE? Inhibitors by Fragment-Based Drug Design.EBI
J Med Chem 61: 2604-2610 (2018)
Second Military Medical University
UNC-51-like Kinase 1: From an Autophagic Initiator to Multifunctional Drug Target.EBI
J Med Chem 61: 6491-6500 (2018)
Sichuan Universitt China Hospital
Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases.EBI
Bioorg Med Chem Lett 28: 1423-1427 (2018)
Ku Leuven
Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.EBI
Eur J Med Chem 150: 9-29 (2018)
Mazandaran University of Medical Sciences
Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors.EBI
Eur J Med Chem 150: 30-38 (2018)
Shandong University
Fragment Based Optimization of Metabotropic Glutamate Receptor 2 (mGluR2) Positive Allosteric Modulators in the Absence of Structural Information.EBI
J Med Chem 62: 234-246 (2019)
Gedeon Richter
Cathepsin B inhibitors: Further exploration of the nitroxoline core.EBI
Bioorg Med Chem Lett 28: 1239-1247 (2018)
University of Ljubljana
4-Amino-7,8-dihydro-1,6-naphthyridin-5(6 H)-ones as Inhaled Phosphodiesterase Type 4 (PDE4) Inhibitors: Structural Biology and Structure-Activity Relationships.EBI
J Med Chem 61: 2472-2489 (2018)
RhôNe-Poulenc Rorer
Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: Inávitro and inávivo evaluation, binding mode prediction and SAR exploration.EBI
Eur J Med Chem 149: 257-268 (2018)
Instituto Oswaldo Cruz
Trypanothione reductase inhibition and anti-leishmanial activity of all-hydrocarbon stapled ?-helical peptides with improved proteolytic stability.EBI
Eur J Med Chem 149: 238-247 (2018)
Instituto De Qu£Mica M£Dica (Iqm-Csic)
Adenosine analogs bearing phosphate isosteres as human MDO1 ligands.EBI
Bioorg Med Chem 26: 1588-1597 (2018)
University of Helsinki
Synthesis and evaluation of 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis.EBI
Bioorg Med Chem 26: 1462-1469 (2018)
Institute of Technology & Science-Pilani
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.EBI
Bioorg Med Chem Lett 28: 987-992 (2018)
Bristol-Myers Squibb
The chemical diversity and structure-based evolution of non-peptide CXCR4 antagonists with diverse therapeutic potential.EBI
Eur J Med Chem 149: 148-169 (2018)
Central South University
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and ?-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.EBI
Bioorg Med Chem 26: 1885-1895 (2018)
Sichuan University
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.EBI
Bioorg Med Chem 26: 1859-1868 (2018)
Shandong University
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.EBI
Bioorg Med Chem 26: 1418-1425 (2018)
Shenyang Pharmaceutical University
Facile synthesis of 1,2-dione-containing abietane analogues for the generation of human carboxylesterase inhibitors.EBI
Eur J Med Chem 149: 79-89 (2018)
St. Jude Children'S Research Hospital
Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor.EBI
Eur J Med Chem 149: 110-121 (2018)
Soochow University
Class I HDAC Inhibitors Display Different Antitumor Mechanism in Leukemia and Prostatic Cancer Cells Depending on Their p53 Status.EBI
J Med Chem 61: 2589-2603 (2018)
Medical University of South Carolina
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.EBI
J Med Chem 61: 2353-2371 (2018)
Chinese Academy of Sciences
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.EBI
J Med Chem 61: 3008-3026 (2018)
Pfizer
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.EBI
J Med Chem 61: 3309-3324 (2018)
Novartis Institutes For Biomedical Research
Discovery and optimization of tetrahydropyrido[4,3-d]pyrimidine derivatives as novel ATX and EGFR dual inhibitors.EBI
Bioorg Med Chem 26: 1784-1796 (2018)
Shenyang Pharmaceutical University
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.EBI
Bioorg Med Chem Lett 28: 1001-1004 (2018)
Alma Mater Studiorum-University of Bologna
Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists.EBI
Eur J Med Chem 149: 30-44 (2018)
Soochow University
Covalent Allosteric Probe for the Metabotropic Glutamate Receptorá2: Design, Synthesis, and Pharmacological Characterization.EBI
J Med Chem 62: 223-233 (2019)
Leiden University
Potent and Selective Inhibitors of Human Sirtuin 5.EBI
J Med Chem 61: 2460-2471 (2018)
Martin-Luther-University Halle-Wittenberg
Structure-Activity Relationship in Monosaccharide-Based Toll-Like Receptor 4 (TLR4) Antagonists.EBI
J Med Chem 61: 2895-2909 (2018)
University of Milano-Bicocca
Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.EBI
Bioorg Med Chem Lett 28: 1043-1049 (2018)
Astrazeneca
Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3K? isoform selective activity.EBI
Bioorg Med Chem Lett 28: 1005-1010 (2018)
India Academy of Scientific & Innovative Research (Acsir)
Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold.EBI
Bioorg Med Chem 26: 1810-1822 (2018)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists.EBI
Bioorg Med Chem 26: 1832-1847 (2018)
Taisho Pharmaceutical
Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.EBI
J Med Chem 61: 2533-2551 (2018)
Sprint Bioscience
Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships.EBI
J Med Chem 61: 2384-2409 (2018)
Takeda Pharmaceutical
Synthesis of 3-aza[4.4.3]propellanes with high ?EBI
Bioorg Med Chem 26: 1705-1712 (2018)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.EBI
Bioorg Med Chem 26: 1797-1809 (2018)
University of Auckland
Synthesis and evaluation of substituted 4-arylimino-3-hydroxybutanoic acids as potential HIV-1 integrase inhibitors.EBI
Bioorg Med Chem Lett 28: 1067-1070 (2018)
Rhodes University
Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists.EBI
Bioorg Med Chem 26: 1598-1608 (2018)
Takeda Pharmaceutical
Pharmacophore requirements for HIV-1 reverse transcriptase inhibitors that selectively "Freeze" the pre-translocated complex during the polymerization catalytic cycle.EBI
Bioorg Med Chem 26: 1713-1726 (2018)
Mcgill University
Novel indanone derivatives as MAO B/HEBI
Eur J Med Chem 148: 487-497 (2018)
Heinrich Heine University Duesseldorf
Synthesis and molecular docking of new roflumilast analogues as preferential-selective potent PDE-4B inhibitors with improved pharmacokinetic profile.EBI
Eur J Med Chem 148: 477-486 (2018)
Cairo University
Discovery of carbazole carboxamides as novel ROR?t inverse agonists.EBI
Eur J Med Chem 148: 465-476 (2018)
Fudan University
Targeting RORs nuclear receptors by novel synthetic steroidal inverse agonists for autoimmune disorders.EBI
Bioorg Med Chem 26: 1686-1704 (2018)
University of Padova
Pan-NS3 protease inhibitors of hepatitis C virus based on an REBI
Eur J Med Chem 148: 453-464 (2018)
Uppsala University
Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead.EBI
Eur J Med Chem 148: 436-452 (2018)
Banaras Hindu University
Precise structures of fucosylated glycosaminoglycan and its oligosaccharides as novel intrinsic factor Xase inhibitors.EBI
Eur J Med Chem 148: 423-435 (2018)
Chinese Academy of Sciences
Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.EBI
Eur J Med Chem 148: 410-422 (2018)
University of Catania
Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation.EBI
Eur J Med Chem 148: 397-409 (2018)
Chungnam National University
Family-wide analysis of aminoacyl-sulfamoyl-3-deazaadenosine analogues as inhibitors of aminoacyl-tRNA synthetases.EBI
Eur J Med Chem 148: 384-396 (2018)
Ku Leuven
Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3K? inhibition.EBI
Bioorg Med Chem 26: 1675-1685 (2018)
Shenyang Pharmaceutical University
Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease.EBI
Bioorg Med Chem 26: 1665-1674 (2018)
China Pharmaceutical University
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.EBI
Bioorg Med Chem 26: 1653-1664 (2018)
Soochow University
Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors.EBI
Bioorg Med Chem 26: 1579-1587 (2018)
Hungarian Academy of Sciences
Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide-Drug Conjugate.EBI
J Med Chem 61: 2052-2061 (2018)
University of California
Ribemansides A and B, TRPC6 Inhibitors from Ribes manshuricum That Suppress TGF-?1-Induced Fibrogenesis in HK-2 Cells.EBI
J Nat Prod 81: 913-917 (2018)
China Pharmaceutical University
New MD2 inhibitors derived from curcumin with improved anti-inflammatory activity.EBI
Eur J Med Chem 148: 291-305 (2018)
Wenzhou Medical University
Novel Tacrine-Hydroxyphenylbenzimidazole hybrids as potential multitarget drug candidates for Alzheimer's disease.EBI
Eur J Med Chem 148: 255-267 (2018)
Universidade De Lisboa
Synthesis and activity towards Alzheimer's disease inávitro: Tacrine, phenolic acid and ligustrazine hybrids.EBI
Eur J Med Chem 148: 238-254 (2018)
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs.EBI
Eur J Med Chem 148: 221-237 (2018)
Xi'An Jiaotong University
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).EBI
J Med Chem 61: 2372-2383 (2018)
Pfizer
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.EBI
J Med Chem 61: 2104-2110 (2018)
University of Edinburgh
Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design.EBI
J Med Chem 61: 2292-2302 (2018)
Vilnius University
Discovery and validation of 2-styryl substituted benzoxazin-4-ones as a novel scaffold for rhomboid protease inhibitors.EBI
Bioorg Med Chem Lett 28: 1417-1422 (2018)
Heinrich-Heine University Duesseldorf
Novel inhibitors of Staphylococcus aureus RnpA that synergize with mupirocin.EBI
Bioorg Med Chem Lett 28: 1127-1131 (2018)
Temple University
CaEBI
J Nat Prod 81: 1070-1074 (2018)
Iwate University
A Systematic Exploration of Macrocyclization in Apelin-13: Impact on Binding, Signaling, Stability, and Cardiovascular Effects.EBI
J Med Chem 61: 2266-2277 (2018)
Universit£
Current Insights of BRAF Inhibitors in Cancer.EBI
J Med Chem 61: 5775-5793 (2018)
Albert Einstein College of Medicine
Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.EBI
J Med Chem 61: 2329-2352 (2018)
University of Auckland
Cyclic peptide inhibitors of lysine-specific demethylase 1 with improved potency identified by alanine scanning mutagenesis.EBI
Eur J Med Chem 148: 210-220 (2018)
Medical University of South Carolina
Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).EBI
Eur J Med Chem 148: 195-209 (2018)
Al-Azhar University
Targeting G-quadruplex DNA structures in the telomere and oncogene promoter regions by benzimidazole?carbazole ligands.EBI
Eur J Med Chem 148: 178-194 (2018)
Indian Institute of Science
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.EBI
Eur J Med Chem 148: 140-153 (2018)
Shanghai Haihe Pharmaceutical
A small group of sulfated benzofurans induces steady-state submaximal inhibition of thrombin.EBI
Bioorg Med Chem Lett 28: 1101-1105 (2018)
Virginia Commonwealth University
Structure-based design and biological evaluation of inhibitors of the pseudomonas aeruginosa heme oxygenase (pa-HemO).EBI
Bioorg Med Chem Lett 28: 1024-1029 (2018)
University of Maryland
Discovery of 1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazoles as novel class of corticotropin releasing factor 1 receptor antagonists.EBI
Bioorg Med Chem 26: 2229-2250 (2018)
Takeda Pharmaceutical
Discovery of novel 4-aryl-thieno[1,4]diazepin-2-one derivatives targeting multiple protein kinases as anticancer agents.EBI
Bioorg Med Chem 26: 1628-1637 (2018)
Hanyang University
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.EBI
J Med Chem 61: 2227-2245 (2018)
Genentech
Synthesis and Biological Evaluation of ( E)-4-Hydroxy-3-methylbut-2-enyl Phosphate (HMBP) Aryloxy Triester Phosphoramidate Prodrugs as Activators of V?9/V?2 T-Cell Immune Responses.EBI
J Med Chem 61: 2111-2117 (2018)
Cardiff University
Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug-Target Interactions.EBI
J Med Chem 62: 24-45 (2019)
Shanghai Jiao Tong University
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.EBI
ACS Med Chem Lett 9: 149-154 (2018)
Xavier University of Louisiana
Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor.EBI
ACS Med Chem Lett 9: 143-148 (2018)
Bristol-Myers Squibb
HTS by NMR for the Identification of Potent and Selective Inhibitors of Metalloenzymes.EBI
ACS Med Chem Lett 9: 137-142 (2018)
University of California-Riverside
Identification of Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors Based on a Phenylimidazole Scaffold.EBI
ACS Med Chem Lett 9: 131-136 (2018)
University Health Network
Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors.EBI
ACS Med Chem Lett 9: 125-130 (2018)
Pfizer
From ROR?t Agonist to Two Types of ROR?t Inverse Agonists.EBI
ACS Med Chem Lett 9: 120-124 (2018)
Fudan University
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.EBI
ACS Med Chem Lett 9: 103-108 (2018)
Glaxosmithkline
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.EBI
ACS Med Chem Lett 9: 98-102 (2018)
Shanghai Hengrui Pharmaceutical
Discovery of 3,3'-Spiro[Azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection.EBI
ACS Med Chem Lett 9: 94-97 (2018)
Wuxi Apptec (Shanghai) Co.
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.EBI
ACS Med Chem Lett 9: 89-93 (2018)
Emory University
-Leucinyl Benzenesulfonamides as Structurally Simplified Leucyl-tRNA Synthetase Inhibitors.EBI
ACS Med Chem Lett 9: 84-88 (2018)
Oxford Drug Design
Nonacidic Chemotype Possessing EBI
ACS Med Chem Lett 9: 78-83 (2018)
Hiroshima International University
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.EBI
ACS Med Chem Lett 9: 68-72 (2018)
Pfizer
Discovery of DSP-1053, a novel benzylpiperidine derivative with potent serotonin transporter inhibitory activity and partial 5-HTEBI
Bioorg Med Chem 26: 1614-1627 (2018)
Sumitomo Dainippon Pharma
Methyllucidone inhibits STAT3 activity by regulating the expression of the protein tyrosine phosphatase MEG2 in DU145 prostate carcinoma cells.EBI
Bioorg Med Chem Lett 28: 853-857 (2018)
Korea University of Science and Technology
Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.EBI
Bioorg Med Chem Lett 28: 841-846 (2018)
Janssen Research and Development
Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.EBI
Bioorg Med Chem Lett 28: 858-862 (2018)
University of Kentucky
Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.EBI
Bioorg Med Chem Lett 28: 847-852 (2018)
China Medical University
Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity.EBI
Eur J Med Chem 148: 95-105 (2018)
Chia Tai Tianqing Pharmaceutical Group
Design, synthesis, and biological evaluation of novel amide and hydrazide based thioether analogs targeting Histone deacteylase (HDAC) enzymes.EBI
Eur J Med Chem 148: 73-85 (2018)
Ahram Canadian University
Synthesis of N-(1-(6-acetamido-5-phenylpyrimidin-4-yl) piperidin-3-yl) amide derivatives as potential inhibitors for mitotic kinesin spindle protein.EBI
Eur J Med Chem 148: 106-115 (2018)
Alagappa University
Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors.EBI
Eur J Med Chem 148: 54-62 (2018)
University of Catania
Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A.EBI
Eur J Med Chem 148: 26-38 (2018)
Universit£
A multidisciplinary study of 3-(?-d-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors.EBI
Eur J Med Chem 147: 266-278 (2018)
University of Debrecen
Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.EBI
Bioorg Med Chem 26: 1495-1510 (2018)
Seoul National University
( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.EBI
J Med Chem 61: 2124-2130 (2018)
University of Siena
Structure-Function Evaluation of Imidazopyridine Derivatives Selective for ?-Subunit-Containing ?-Aminobutyric Acid Type A (GABAEBI
J Med Chem 61: 1951-1968 (2018)
Johannes Gutenberg University Mainz
Investigating PKA-RII specificity using analogs of the PKA:AKAP peptide inhibitor STAD-2.EBI
Bioorg Med Chem 26: 1174-1178 (2018)
University of Georgia
Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.EBI
Eur J Med Chem 147: 238-252 (2018)
Guangzhou Medical University
Positive and Negative Allosteric Modulators of N-Methyl-d-aspartate (NMDA) Receptors: Structure-Activity Relationships and Mechanisms of Action.EBI
J Med Chem 62: 3-23 (2019)
University of Bristol
A Structure-Activity Relationship Study of Bitopic NEBI
J Med Chem 61: 2087-2103 (2018)
Monash University
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR)?/?/? Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.EBI
J Med Chem 61: 2246-2265 (2018)
Inventiva
Exploiting the S4-S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis.EBI
J Med Chem 61: 1858-1870 (2018)
University of Tours
New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma and embryonic carcinoma cells.EBI
Bioorg Med Chem 26: 1523-1537 (2018)
University of Nevada
Probing biological activity through structural modelling of ligand-receptor interactions of 2,4-disubstituted thiazole retinoids.EBI
Bioorg Med Chem 26: 1560-1572 (2018)
Helwan University
Discovery of morpholine-based aryl sulfonamides as NaEBI
Bioorg Med Chem Lett 28: 958-962 (2018)
Bristol-Myers Squibb Research and Development
MF-8, a novel promising arylpiperazine-hydantoin based 5-HTEBI
Bioorg Med Chem Lett 28: 878-883 (2018)
Jagiellonian University Medical College
Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.EBI
Eur J Med Chem 147: 227-237 (2018)
Guangdong Medical University
Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors.EBI
Eur J Med Chem 147: 194-204 (2018)
Anhui Medical University
High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein-Protein Interaction.EBI
J Med Chem 61: 1934-1950 (2018)
Zhejiang University
Tozasertib Analogues as Inhibitors of Necroptotic Cell Death.EBI
J Med Chem 61: 1895-1920 (2018)
University of Antwerp
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.EBI
Bioorg Med Chem Lett 28: 906-909 (2018)
Novartis Institutes For Biomedical Research
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.EBI
Bioorg Med Chem Lett 28: 934-941 (2018)
Frost Biologic
Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase.EBI
Bioorg Med Chem Lett 28: 922-925 (2018)
Sanofi-Aventis Deutschland
Synthesis of polyozellin, a prolyl oligopeptidase inhibitor, and its structural revision.EBI
Bioorg Med Chem Lett 28: 930-933 (2018)
Riken Csrs
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships.EBI
Bioorg Med Chem Lett 28: 974-978 (2018)
Beijing University of Technology
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.EBI
Bioorg Med Chem 26: 1511-1522 (2018)
Prin. K. M. Kundnani College of Pharmacy
Discovery of chromenes as inhibitors of macrophage migration inhibitory factor.EBI
Bioorg Med Chem 26: 999-1005 (2018)
University of Groningen
Synthesis and biological evaluation of novel quinazoline-4-piperidinesulfamide derivatives as inhibitors of NPP1.EBI
Eur J Med Chem 147: 130-149 (2018)
Universit£
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.EBI
Bioorg Med Chem Lett 28: 952-957 (2018)
National Research Centre
Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine ?-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation.EBI
Bioorg Med Chem Lett 28: 1111-1115 (2018)
Amgen
O6C-20-nor-salvinorin A is a stable and potent KOR agonist.EBI
Bioorg Med Chem Lett 28: 2770-2772 (2018)
The Scripps Research Institute
Design, synthesis, and biological evaluation of inhibitors of the NADPH oxidase, Nox4.EBI
Bioorg Med Chem 26: 989-998 (2018)
Emory University
Recent updates for designing CCR5 antagonists as anti-retroviral agents.EBI
Eur J Med Chem 147: 115-129 (2018)
Nirma University
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HTEBI
Eur J Med Chem 147: 102-114 (2018)
Jagiellonian University Medical College
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor ? and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.EBI
J Med Chem 61: 2027-2040 (2018)
Duquesne University
Selective Inhibitors of Human Neuraminidase 3.EBI
J Med Chem 61: 1990-2008 (2018)
University of Alberta
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.EBI
J Med Chem 61: 1785-1799 (2018)
Astrazeneca
Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on ?EBI
Bioorg Med Chem Lett 28: 547-551 (2018)
Guangzhou Medical University
Discovery of novel potent HCV NS5B polymerase non-nucleoside inhibitors bearing a fused benzofuran scaffold.EBI
Bioorg Med Chem Lett 28: 963-968 (2018)
Presidio Pharmaceuticals
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGF?RI).EBI
Bioorg Med Chem 26: 1026-1034 (2018)
Bristol-Myers Squibb
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.EBI
Eur J Med Chem 147: 77-89 (2018)
Shaanxi Normal University
Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates.EBI
Eur J Med Chem 147: 48-65 (2018)
Federal University of Alfenas
Targeting polyamine transport in Trypanosoma cruzi.EBI
Eur J Med Chem 147: 1-6 (2018)
Universidad De Buenos Aires
Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy.EBI
J Med Chem 61: 5794-5804 (2018)
Fudan University
Activation loop targeting strategy for design of receptor-interacting protein kinase 2 (RIPK2) inhibitors.EBI
Bioorg Med Chem Lett 28: 577-583 (2018)
University of Houston
Fluorous-tag assisted synthesis of a glycosaminoglycan mimetic tetrasaccharide as a high-affinity FGF-2 and midkine ligand.EBI
Bioorg Med Chem 26: 1076-1085 (2018)
Csic and Universidad De Sevilla
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.EBI
Bioorg Med Chem 26: 1102-1115 (2018)
Sichuan University
Regioselective synthesis of 7-O-esters of the flavonolignan silibinin and SARs lead to compounds with overadditive neuroprotective effects.EBI
Eur J Med Chem 146: 93-107 (2018)
Julius-Maximilians-Universit£T W£Rzburg
Part III: Novel checkpoint kinase 2 (Chk2) inhibitors; design, synthesis and biological evaluation of pyrimidine-benzimidazole conjugates.EBI
Eur J Med Chem 146: 687-708 (2018)
National Research Centre
Design, synthesis and biological evaluation of 1-hydroxy-2-phenyl-4-pyridyl-1H-imidazole derivatives as xanthine oxidase inhibitors.EBI
Eur J Med Chem 146: 668-677 (2018)
Shenyang Pharmaceutical University
Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.EBI
Eur J Med Chem 146: 636-650 (2018)
Nagahama Institute of Bio-Science and Technology
Effects of rigidity on the selectivity of protein kinase inhibitors.EBI
Eur J Med Chem 146: 519-528 (2018)
University of Southern California
Structure activity relationships, multidrug resistance reversal and selectivity of heteroarylphenyl ABCG2 inhibitors.EBI
Eur J Med Chem 146: 483-500 (2018)
Rheinische Friedrich-Wilhelms-Universit£T Bonn
Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents.EBI
Eur J Med Chem 146: 471-482 (2018)
Hunan Provinc
Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII.EBI
Eur J Med Chem 146: 47-59 (2018)
Universit£
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?.EBI
Eur J Med Chem 146: 460-470 (2018)
Shenyang Pharmaceutical University
High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.EBI
Eur J Med Chem 146: 451-459 (2018)
Nanjing Forestry University
Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.EBI
Eur J Med Chem 146: 423-434 (2018)
University of Modena and Reggio Emilia
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.EBI
Eur J Med Chem 146: 381-394 (2018)
Jagiellonian University
Identification of novel NEBI
Eur J Med Chem 146: 368-380 (2018)
Zhuhai Campus of Zunyi Medical University
An overview on crystal structures of InhA protein: Apo-form, in complex with its natural ligands and inhibitors.EBI
Eur J Med Chem 146: 318-343 (2018)
Cnrs
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.EBI
Eur J Med Chem 146: 299-317 (2018)
Hefei University of Technology
Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.EBI
Eur J Med Chem 146: 287-298 (2018)
Jiangxi University of Traditional Chinese Medicine
Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.EBI
Eur J Med Chem 146: 260-273 (2018)
Aljouf University
Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway.EBI
Eur J Med Chem 146: 251-259 (2018)
China Pharmaceutical University
Design, semisynthesis, ?-glucosidase inhibitory, cytotoxic, and antibacterial activities of p-terphenyl derivatives.EBI
Eur J Med Chem 146: 232-244 (2018)
Ocean University of China
Discovery of C-1 modified oseltamivir derivatives as potent influenza neuraminidase inhibitors.EBI
Eur J Med Chem 146: 220-231 (2018)
Shandong University
Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-?).EBI
Eur J Med Chem 146: 206-219 (2018)
Central University of Punjab
Rational design, chemical synthesis and biological evaluation of novel biguanides exploring species-specificity responsiveness of TAAR1 agonists.EBI
Eur J Med Chem 146: 171-184 (2018)
University of Genoa
Synthesis and biological evaluation of pyridazinone derivatives as potential anti-inflammatory agents.EBI
Eur J Med Chem 146: 139-146 (2018)
Universit£
First homology model of Plasmodium falciparum glucose-6-phosphate dehydrogenase: Discovery of selective substrate analog-based inhibitors as novel antimalarial agents.EBI
Eur J Med Chem 146: 108-122 (2018)
University of Barcelona
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.EBI
Eur J Med Chem 145: 790-804 (2018)
Jagiellonian University Medical College
Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.EBI
Eur J Med Chem 145: 770-789 (2018)
University of Otago
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.EBI
J Med Chem 61: 2518-2532 (2018)
Gsk Pharmaceuticals R & D
Metabolomics-Guided Discovery of Microginin Peptides from Cultures of the Cyanobacterium Microcystis aeruginosa.EBI
J Nat Prod 81: 349-355 (2018)
University of North Carolina Wilmington
Synthesis of novel multivalent fluorescent inhibitors with high affinity to prostate cancer and their biological evaluation.EBI
Bioorg Med Chem Lett 28: 572-576 (2018)
Yonsei University College of Medicine
Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A.EBI
Bioorg Med Chem 26: 1225-1231 (2018)
The University of Tokyo
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.EBI
J Med Chem 61: 5822-5880 (2018)
Bristol-Myers Squibb
Mucroniferanines A-G, Isoquinoline Alkaloids from Corydalis mucronifera.EBI
J Nat Prod 81: 364-370 (2018)
Peking University
Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles.EBI
J Med Chem 61: 1646-1663 (2018)
Julius Maximilian University of W£Rzburg
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.EBI
J Med Chem 61: 1622-1635 (2018)
Novartis Institutes For Biomedical Research
Structural development of tetrachlorophthalimides as liver X receptor ? (LXR?)-selective agonists with improved aqueous solubility.EBI
Bioorg Med Chem Lett 28: 796-801 (2018)
The University of Tokyo
A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: Synthesis, biological investigation and docking studies.EBI
Bioorg Med Chem Lett 28: 651-657 (2018)
Universit£
Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.EBI
Bioorg Med Chem Lett 28: 732-736 (2018)
Bristol-Myers Squibb Research and Development
Semisynthesis and biological evaluation of a cotylenin A mimic derived from fusicoccin A.EBI
Bioorg Med Chem Lett 28: 646-650 (2018)
Osaka University
Synthesis, kinetics and inhibition of Escherichia coli Heptosyltransferase I by monosaccharide analogues of Lipid A.EBI
Bioorg Med Chem Lett 28: 594-600 (2018)
Wesleyan University
2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPAR? partial agonism.EBI
Bioorg Med Chem 26: 1069-1075 (2018)
Seoul National University
Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region.EBI
Bioorg Med Chem 26: 1035-1049 (2018)
Seoul National University
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.EBI
Bioorg Med Chem 26: 913-924 (2018)
Astrazeneca
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.EBI
J Med Chem 61: 1969-1989 (2018)
University of Paris
Structural and Functional Analysis of Anti-Influenza Activity of 4-, 7-, 8- and 9-Deoxygenated 2,3-Difluoro- N-acetylneuraminic Acid Derivatives.EBI
J Med Chem 61: 1921-1933 (2018)
Csiro Manufacturing
Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.EBI
Eur J Med Chem 146: 79-92 (2018)
Minia University
Novel inhibitors of the rRNA ErmC' methyltransferase to block resistance to macrolides, lincosamides, streptogramine B antibiotics.EBI
Eur J Med Chem 146: 60-67 (2018)
International Institute of Molecular and Cell Biology
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.EBI
Bioorg Med Chem Lett 28: 606-611 (2018)
University of Chinese Academy of Sciences
Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells.EBI
Bioorg Med Chem Lett 28: 700-706 (2018)
Tianjin International Joint Academy of Biomedicine
Selective inhibition of monoamine oxidase A by hispidol.EBI
Bioorg Med Chem Lett 28: 584-588 (2018)
Sunchon National University
Cyclizidine-Type Alkaloids from Streptomyces sp. HNA39.EBI
J Nat Prod 81: 394-399 (2018)
Zhejiang University
New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model.EBI
J Med Chem 61: 1595-1608 (2018)
University of Belgrade
Dual Nicotinic Acetylcholine Receptor ?4?2 Antagonists/?7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.EBI
J Med Chem 61: 1719-1729 (2018)
University of Copenhagen
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.EBI
J Med Chem 61: 1355-1374 (2018)
Hec Pharma Group
Probing the Antiallergic and Anti-inflammatory Activity of Biflavonoids and Dihydroflavonols from Dietes bicolor.EBI
J Nat Prod 81: 243-253 (2018)
Ain Shams University
The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaEBI
J Med Chem 61: 1730-1736 (2018)
The University of Queensland
Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.EBI
ACS Med Chem Lett 8: 1183-1187 (2017)
Institute For Research In Cancer and Allied Diseases
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.EBI
Bioorg Med Chem 26: 891-902 (2018)
Delhi Institute of Pharmaceutical Sciences and Research (Dipsar)
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.EBI
Bioorg Med Chem 26: 903-912 (2018)
Shanghai Jiao Tong University
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.EBI
J Med Chem 61: 1664-1687 (2018)
Csir-Indian Institute of Integrative Medicine
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.EBI
Bioorg Med Chem Lett 28: 711-719 (2018)
Janssen Infectious Diseases Diagnostics
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.EBI
Bioorg Med Chem Lett 28: 762-768 (2018)
University of California Davis
Discovery of a novel potent GPR40 full agonist.EBI
Bioorg Med Chem Lett 28: 720-726 (2018)
Janssen Research & Developmen
Identification of novel plasminogen activator inhibitor-1 inhibitors with improved oral bioavailability: Structure optimization of N-acylanthranilic acid derivatives.EBI
Bioorg Med Chem Lett 28: 809-813 (2018)
Hamari Chemicals
Binding-Site Compatible Fragment Growing Applied to the Design of ?EBI
J Med Chem 61: 1118-1129 (2018)
Philipps-University Marburg
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.EBI
J Med Chem 61: 5467-5483 (2018)
Sun Yat-Sen University
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.EBI
J Med Chem 61: 1552-1575 (2018)
A*Star
Development of novel oxazolo[5,4-d]pyrimidines as competitive CBEBI
Eur J Med Chem 146: 68-78 (2018)
Univ. Lille
Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo.EBI
J Med Chem 61: 865-880 (2018)
The Genomics Institute of The Novartis Research Foundation
Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold.EBI
Eur J Med Chem 145: 805-812 (2018)
Sun Yat-Sen University
Design, synthesis and biological evaluation of new carbazole derivatives as anti-cancer and anti-migratory agents.EBI
Bioorg Med Chem 26: 884-890 (2018)
University of Puerto Rico
Salutaxel, a Conjugate of Docetaxel and a Muramyl Dipeptide (MDP) Analogue, Acts as Multifunctional Prodrug That Inhibits Tumor Growth and Metastasis.EBI
NA
Shenzhen Salubris Pharmaceuticals Co.
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.EBI
J Med Chem 61: 1499-1518 (2018)
China Pharmaceutical University
Tetrahydroacridine derivatives with dichloronicotinic acid moiety as attractive, multipotent agents for Alzheimer's disease treatment.EBI
Eur J Med Chem 145: 760-769 (2018)
Medical University of Lodz
Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.EBI
Eur J Med Chem 145: 726-734 (2018)
Fudan University
Bysspectin A, an unusual octaketide dimer and the precursor derivatives from the endophytic fungus Byssochlamys spectabilis IMM0002 and their biological activities.EBI
Eur J Med Chem 145: 717-725 (2018)
Chinese Academy of Medical Sciences and Peking Union Medical College
Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.EBI
Eur J Med Chem 145: 673-690 (2018)
Seoul National University
Synthesis and anti-tumor activity of EF24 analogues as IKK? inhibitors.EBI
Eur J Med Chem 144: 218-228 (2018)
The First Affiliated Hospital of Wenzhou Medical University
Synthesis and Pharmacological Characterization of C4EBI
J Med Chem 61: 2303-2328 (2018)
TBA
Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties.EBI
J Med Chem 61: 946-979 (2018)
Emory University
Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution.EBI
ACS Med Chem Lett 9: 51-55 (2018)
Longwood University
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.EBI
ACS Med Chem Lett 9: 39-44 (2018)
Merck Research Laboratories
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.EBI
ACS Med Chem Lett 9: 34-38 (2018)
Second Military Medical University
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.EBI
ACS Med Chem Lett 9: 28-33 (2018)
Abbvie
Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists.EBI
ACS Med Chem Lett 9: 17-22 (2018)
Emory University
Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application.EBI
ACS Med Chem Lett 9: 6-10 (2018)
Tokyo Medical and Dental University
Structure-based development of an osteoprotegerin-like glycopeptide that blocks RANKL/RANK interactions and reduces ovariectomy-induced bone loss in mice.EBI
Eur J Med Chem 145: 661-672 (2018)
Second Military Medical University
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.EBI
Eur J Med Chem 145: 606-621 (2018)
Pfizer
?-Amino-?-carboxymuconate-?-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De Novo Nicotinamide Adenine Dinucleotide (NADEBI
J Med Chem 61: 745-759 (2018)
Tes Pharma
Identification of novel quinazolinedione derivatives as ROR?t inverse agonist.EBI
Bioorg Med Chem 26: 721-736 (2018)
Takeda Pharmaceutical
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.EBI
J Med Chem 61: 1074-1085 (2018)
The University of Arizona
Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.EBI
Eur J Med Chem 145: 588-593 (2018)
Hefei University of Technology
Structure-based design of human immuno- and constitutive proteasomes inhibitors.EBI
Eur J Med Chem 145: 570-587 (2018)
Universit£
Synthesis of deuterium-labelled analogues of NLRP3 inflammasome inhibitor MCC950.EBI
Bioorg Med Chem Lett 28: 793-795 (2018)
The University of Queensland
Essential structure of orexin 1 receptor antagonist YNT-707, Part II: Drastic effect of the 14-hydroxy group on the orexin 1 receptor antagonistic activity.EBI
Bioorg Med Chem Lett 28: 774-777 (2018)
University of Tsukuba
Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis.EBI
Bioorg Med Chem Lett 28: 787-792 (2018)
Universit£
Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.EBI
Bioorg Med Chem Lett 28: 748-755 (2018)
Novartis Institutes For Biomedical Research
Inávivo potent BM635 analogue with improved drug-like properties.EBI
Eur J Med Chem 145: 539-550 (2018)
Sapienza University of Rome
Synthesis and biological evaluation of novel bavachinin analogs as anticancer agents.EBI
Eur J Med Chem 145: 511-523 (2018)
Csir-Indian Institute of Integrative Medicine
Privileged scaffolds as MAO inhibitors: Retrospect and prospects.EBI
NA
Babu Banarasi Das Northern India Institute of Technology
Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.EBI
Eur J Med Chem 145: 431-444 (2018)
University of S£O Paulo
Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.EBI
Eur J Med Chem 145: 413-424 (2018)
Tiumbio
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.EBI
Eur J Med Chem 145: 389-403 (2018)
Chinese Academy of Sciences
Synthesis and bioevaluation and doking study of 1H-pyrrolo[2,3-b]pyridine derivatives bearing aromatic hydrazone moiety as c-Met inhibitors.EBI
Eur J Med Chem 145: 315-327 (2018)
Jiangxi Science & Technology Normal University
Design, synthesis and evaluation of ?-turn mimetics as LSD1-selective inhibitors.EBI
Bioorg Med Chem 26: 775-785 (2018)
Kyoto Prefectural University of Medicine
Identification and initial optimization of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB).EBI
Bioorg Med Chem Lett 28: 756-761 (2018)
Genesis Biotechnology Group
Theoretical research in structure characteristics of different inhibitors and differences of binding modes with CBP bromodomain.EBI
Bioorg Med Chem 26: 712-720 (2018)
Jilin University
Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.EBI
Eur J Med Chem 153: 2-28 (2018)
Abdul Wali Khan University Mardan
Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.EBI
Bioorg Med Chem Lett 28: 769-773 (2018)
Semmelweis University
Development of potent and proteolytically stable human neuromedin U receptor agonists.EBI
Eur J Med Chem 144: 887-897 (2018)
Vrije Universiteit Brussel
Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation.EBI
Eur J Med Chem 145: 273-290 (2018)
Bahcesehir University (Bau)
Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.EBI
Eur J Med Chem 145: 235-251 (2018)
East China University of Science and Technology
X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential.EBI
J Med Chem 61: 1276-1284 (2018)
Rheinische Friedrich-Wilhelms-Universit£T
Phenylthiomethyl Ketone-Based Fragments Show Selective and Irreversible Inhibition of Enteroviral 3C Proteases.EBI
J Med Chem 61: 1218-1230 (2018)
Freie Universit£T Berlin
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.EBI
Eur J Med Chem 145: 96-112 (2018)
Sichuan University and Collaborative Innovation Center
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.EBI
Eur J Med Chem 145: 74-85 (2018)
Shanghai Institute of Materia Medica
Peramivir conjugates as orally available agents against influenza H275Y mutant.EBI
Eur J Med Chem 145: 224-234 (2018)
National Taiwan University
Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine "bio-oxidizable" prodrugs: Synthesis, biological evaluation and structure-activity relationship.EBI
Eur J Med Chem 145: 165-190 (2018)
Vfp Therapies
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.EBI
J Med Chem 61: 2410-2421 (2018)
Vanderbilt University School of Medicine
Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).EBI
J Med Chem 61: 1541-1551 (2018)
Icahn School of Medicine At Mount Sinai
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.EBI
Bioorg Med Chem 26: 747-757 (2018)
Nanjing University of Chinese Medicine
Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide.EBI
Bioorg Med Chem 26: 845-854 (2018)
China Pharmaceutical University
Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold.EBI
Bioorg Med Chem 26: 581-589 (2018)
Shanghai Hengrui Pharmaceutical
Part II: New candidates of pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors.EBI
Eur J Med Chem 144: 859-873 (2018)
National Research Centre
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.EBI
J Med Chem 61: 681-694 (2018)
Bristol-Myers Squibb
Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.EBI
J Med Chem 61: 818-833 (2018)
National Health Research Institutes
Interfering with HuR-RNA Interaction: Design, Synthesis and Biological Characterization of Tanshinone Mimics as Novel, Effective HuR Inhibitors.EBI
J Med Chem 61: 1483-1498 (2018)
Institute of Molecular Science and Technology (Istm)
Synthesis and Biological Evaluation of Calothrixins B and their Deoxygenated Analogues.EBI
J Med Chem 61: 1285-1315 (2018)
University of Madras
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.EBI
J Med Chem 61: 1340-1354 (2018)
University of Ferrara
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.EBI
J Med Chem 61: 881-904 (2018)
Nankai University
Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions.EBI
Eur J Med Chem 144: 843-858 (2018)
National Institute of Pharmaceutical Education and Research (NIPER)
Inhibition of protein tyrosine phosphatase 1B (PTP1B) and ?-glucosidase by xanthones from Cratoxylum cochinchinense, and their kinetic characterization.EBI
Bioorg Med Chem 26: 737-746 (2018)
Gyeongsang National University
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.EBI
Bioorg Med Chem 26: 637-646 (2018)
Chinese Academy of Medical Sciences and Peking Union Medical College
Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors.EBI
Bioorg Med Chem 26: 675-687 (2018)
Vilnius University
(N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo.EBI
J Med Chem 61: 905-917 (2018)
Taipei Medical University
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.EBI
J Med Chem 61: 1061-1073 (2018)
Astrazeneca
Isolation of Flavonoids and Flavonoid Glycosides from Myrsine africana and Their Inhibitory Activities against Mushroom Tyrosinase.EBI
J Nat Prod 81: 49-56 (2018)
University of Pretoria
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.EBI
J Med Chem 61: 1086-1097 (2018)
Pfizer
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.EBI
J Med Chem 61: 1130-1152 (2018)
Pfizer
Emerging New Targets for the Treatment of Resistant Fungal Infections.EBI
J Med Chem 61: 5484-5511 (2018)
Second Military Medical University
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.EBI
J Med Chem 61: 1001-1018 (2018)
Pfizer
Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.EBI
J Med Chem 61: 5450-5466 (2018)
University of Sharjah
Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.EBI
Bioorg Med Chem 26: 703-711 (2018)
Guangdong Pharmaceutical University
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.EBI
Bioorg Med Chem 26: 647-660 (2018)
Takeda Pharmaceutical
Structural optimization of NEBI
Bioorg Med Chem 26: 661-674 (2018)
Universit£
Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.EBI
Eur J Med Chem 144: 758-766 (2018)
Sun Yat-Sen University
Novel non-sulfonamide 5-HTEBI
Eur J Med Chem 144: 716-729 (2018)
Palack£
Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HTEBI
Eur J Med Chem 144: 701-715 (2018)
Shanghai Institute of Pharmaceutical Industry
Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase?4 Isoform Inhibitors for Male Contraception.EBI
J Med Chem 61: 1800-1820 (2018)
University of Minnesota
Neutral Porphyrin Derivative Exerts Anticancer Activity by Targeting Cellular Topoisomerase I (Top1) and Promotes Apoptotic Cell Death without Stabilizing Top1-DNA Cleavage Complexes.EBI
J Med Chem 61: 804-817 (2018)
Ahmedabad University
Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site.EBI
Eur J Med Chem 144: 692-700 (2018)
Qilu University of Technology
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.EBI
Eur J Med Chem 144: 672-681 (2018)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.EBI
Eur J Med Chem 144: 635-650 (2018)
Alexandria University
Synthesis of (3S,4S,5S)-trihydroxylpiperidine derivatives as enzyme stabilizers to improve therapeutic enzyme activity in Fabry patient cell lines.EBI
Eur J Med Chem 144: 626-634 (2018)
National Yang-Ming University
Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.EBI
Eur J Med Chem 144: 612-625 (2018)
Goethe University
Design, synthesis and biological evaluation of novel pyridine-thiazolidinone derivatives as anticancer agents: Targeting human carbonic anhydrase IX.EBI
Eur J Med Chem 144: 544-556 (2018)
Jamia Millia Islamia
Development of dual casein kinase 1?/1? (CK1?/?) inhibitors for treatment of breast cancer.EBI
Bioorg Med Chem 26: 590-602 (2018)
Scripps Florida
Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy.EBI
Eur J Med Chem 144: 517-528 (2018)
Sichuan University
Recent advance in oxazole-based medicinal chemistry.EBI
NA
Linyi University
Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors.EBI
Eur J Med Chem 144: 424-434 (2018)
Xuzhou Medical University
A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors.EBI
Eur J Med Chem 144: 410-423 (2018)
Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Cibican)
Development of novel ?-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.EBI
Eur J Med Chem 144: 398-409 (2018)
Nantong University
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.EBI
Eur J Med Chem 144: 386-397 (2018)
Shanghai Institute of Materia Medica (Simm)
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.EBI
Bioorg Med Chem 26: 798-814 (2018)
King'S College
Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (?EBI
Eur J Med Chem 144: 359-371 (2018)
Universit£
Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity.EBI
J Med Chem 61: 1164-1175 (2018)
Lund University
Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma.EBI
J Med Chem 61: 695-710 (2018)
Oncoarendi Therapeutics
Phenanthrenes: A Promising Group of Plant Secondary Metabolites.EBI
NA
University of Szeged
Antiobesity and emetic effects of a short-length peptide YY analog and its PEGylated and alkylated derivatives.EBI
Bioorg Med Chem 26: 566-572 (2018)
Takeda Pharmaceutical
Synthesis and biological evaluation of 6-substituted-5-fluorouridine ProTides.EBI
Bioorg Med Chem 26: 551-565 (2018)
Cardiff University
Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers.EBI
Bioorg Med Chem 26: 603-608 (2018)
Hiroshima University
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.EBI
Eur J Med Chem 144: 349-358 (2018)
University of Perugia
Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.EBI
Eur J Med Chem 144: 330-348 (2018)
Ain Shams University
Development of inhibitors of receptor protein tyrosine phosphatase ?/? (PTPRZ1) as candidates for CNS disorders.EBI
Eur J Med Chem 144: 318-329 (2018)
Universidad San Pablo-Ceu
Naturally occurring Diels-Alder-type adducts from Morus nigra as potent inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase B.EBI
Eur J Med Chem 144: 277-288 (2018)
Universidade Federal De Santa Catarina
Synthesis, structure-activity relationships, and mechanistic studies of 5-arylazo-tropolone derivatives as novel xanthine oxidase (XO) inhibitors.EBI
Bioorg Med Chem 26: 536-542 (2018)
Tohoku Medical and Pharmaceutical University
1,3,5-triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity.EBI
Eur J Med Chem 144: 262-276 (2018)
National University of Singapore
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.EBI
Bioorg Med Chem 26: 309-339 (2018)
University of Kwazulu-Natal
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).EBI
Bioorg Med Chem 26: 1157-1161 (2018)
University of Kansas
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.EBI
Eur J Med Chem 144: 201-210 (2018)
Cnrs Upr 4301
Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.EBI
Eur J Med Chem 144: 179-200 (2018)
University of Genoa
Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.EBI
J Med Chem 61: 724-733 (2018)
University of Oxford
In Silico Fragment-Based Design Identifies Subfamily B1 Metallo-?-lactamase Inhibitors.EBI
J Med Chem 61: 1255-1260 (2018)
University of Leeds
Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir.EBI
J Med Chem 61: 62-80 (2018)
Bristol-Myers Squibb Research and Development
Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase.EBI
J Med Chem 61: 1182-1203 (2018)
Scynexis
5-HTEBI
Bioorg Med Chem 26: 527-535 (2018)
Medical University of Warsaw
Antagonists of the adenosine AEBI
Eur J Med Chem 144: 151-163 (2018)
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer
Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity.EBI
Eur J Med Chem 144: 128-136 (2018)
Henan University
2-Substituted 7-trifluoromethyl-thiadiazolopyrimidones as alkaline phosphatase inhibitors. Synthesis, structure activity relationship and molecular docking study.EBI
Eur J Med Chem 144: 116-127 (2018)
Universit£T Rostock
High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target.EBI
J Med Chem 61: 5093-5107 (2018)
The Feinstein Institute For Medical Research
"Seriously Sweet": Acesulfame K Exhibits Selective Inhibition Using Alternative Binding Modes in Carbonic Anhydrase Isoforms.EBI
J Med Chem 61: 1176-1181 (2018)
University of Florida
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?EBI
J Med Chem 61: 5073-5092 (2018)
University of South Australia
Discovery of orally efficacious ROR?t inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.EBI
Bioorg Med Chem 26: 483-500 (2018)
Takeda Pharmaceutical
SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.EBI
ACS Med Chem Lett 8: 1336-1340 (2017)
Sungkyunkwan University
VU6010608, a Novel mGluEBI
ACS Med Chem Lett 8: 1326-1330 (2017)
Vanderbilt University
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.EBI
ACS Med Chem Lett 8: 1320-1325 (2017)
Japan Tobacco
Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases.EBI
ACS Med Chem Lett 8: 1314-1319 (2017)
University of Florence
Discovery of APD371: Identification of a Highly Potent and Selective CBEBI
ACS Med Chem Lett 8: 1309-1313 (2017)
Arena Pharmaceuticals
Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.EBI
ACS Med Chem Lett 8: 1304-1308 (2017)
Merck
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.EBI
ACS Med Chem Lett 8: 1298-1303 (2017)
Walter and Eliza Hall Institute of Medical Research
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.EBI
ACS Med Chem Lett 8: 1292-1297 (2017)
Merck
Adding a Hydrogen Bond May Not Help: Naphthyridinone vs Quinoline Inhibitors of Macrophage Migration Inhibitory Factor.EBI
ACS Med Chem Lett 8: 1287-1291 (2017)
Yale University
Discovery of a Slow Tight Binding LPA1 Antagonist (ONO-0300302) for the Treatment of Benign Prostatic Hyperplasia.EBI
ACS Med Chem Lett 8: 1281-1286 (2017)
Ono Pharmaceutical
Identification of an Indazole-Based Pharmacophore for the Inhibition of FGFR Kinases Using Fragment-Led EBI
ACS Med Chem Lett 8: 1264-1268 (2017)
University of Leeds
HTS and Structure Based Optimization of Indazole-Derived ULK1 Inhibitors.EBI
ACS Med Chem Lett 8: 1258-1263 (2017)
The Scripps Research Institute
Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.EBI
ACS Med Chem Lett 8: 1252-1257 (2017)
Boehringer Ingelheim Pharma
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.EBI
ACS Med Chem Lett 8: 1246-1251 (2017)
Wuxi Apptec (Shanghai)
2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine ?-Lyase (CSE).EBI
ACS Med Chem Lett 8: 1241-1245 (2017)
University of Illinois At Chicago
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.EBI
ACS Med Chem Lett 8: 1224-1229 (2017)
Vertex Pharmaceuticals
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.EBI
ACS Med Chem Lett 8: 1218-1223 (2017)
Alma Mater Studiorum-University of Bologna
Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors.EBI
ACS Med Chem Lett 8: 1213-1217 (2017)
University of Florence
Ubiquitin-Specific Inhibitors for the Treatment of Cancers, Autoimmune, and Infectious Diseases.EBI
ACS Med Chem Lett 8: 1211-1212 (2017)
Usona Institute
Discovery of orally efficacious ROR?t inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.EBI
Bioorg Med Chem 26: 470-482 (2018)
Takeda Pharmaceutical
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective AEBI
J Med Chem 61: 305-318 (2018)
University of Camerino
7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of?-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.EBI
J Med Chem 61: 251-264 (2018)
University of Li£Ge
Current knowledge on the nucleotide agonists for the P2Y2 receptor.EBI
Bioorg Med Chem 26: 366-375 (2018)
China Pharmaceutical University
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.EBI
Bioorg Med Chem 26: 501-508 (2018)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Targeting protein-protein interaction between MLL1 and reciprocal proteins for leukemia therapy.EBI
Bioorg Med Chem 26: 356-365 (2018)
China Pharmaceutical University
Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.EBI
Bioorg Med Chem Lett 28: 979-984 (2018)
Boehringer Ingelheim Pharmaceuticals
Structure-Guided Synthesis and Mechanistic Studies Reveal Sweetspots on Naphthyl Salicyl Hydrazone Scaffold as Non-Nucleosidic Competitive, Reversible Inhibitors of Human Ribonucleotide Reductase.EBI
J Med Chem 61: 666-680 (2018)
Case Western Reserve University
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.EBI
J Med Chem 61: 834-864 (2018)
St. John'S University
Targeting Transcriptional Enhanced Associate Domains (TEADs).EBI
J Med Chem 61: 5057-5072 (2018)
Universities of Lille
Discovery of novel scaffolds for ?-secretase modulators without an arylimidazole moiety.EBI
Bioorg Med Chem 26: 435-442 (2018)
Astellas Pharma
Design, synthesis and biological assessment of new thiazolylhydrazine derivatives as selective and reversible hMAO-A inhibitors.EBI
Eur J Med Chem 144: 68-81 (2018)
Anadolu University
?-Methylation enhances the potency of isoprenoid triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.EBI
Bioorg Med Chem 26: 376-385 (2018)
University of Iowa
NOTA analogue: A first dithiocarbamate inhibitor of metallo-?-lactamases.EBI
Bioorg Med Chem Lett 28: 214-221 (2018)
Zhengzhou University
Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.EBI
Eur J Med Chem 144: 52-67 (2018)
University of Freiburg
Synthesis and biological evaluation of novel 1-(aryl-aldehyde-oxime)uracil derivatives as a new class of thymidine phosphorylase inhibitors.EBI
Eur J Med Chem 144: 41-51 (2018)
Yunnan University
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.EBI
Eur J Med Chem 144: 1-28 (2018)
Beijing Normal University
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).EBI
J Med Chem 61: 1204-1217 (2018)
Icahn School of Medicine At Mount Sinai
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.EBI
J Med Chem 61: 224-250 (2018)
East China University of Science and Technology
Selective inhibition of ?-N-acetylhexosaminidases by thioglycosyl-naphthalimide hybrid molecules.EBI
Bioorg Med Chem 26: 394-400 (2018)
Dalian University of Technology
Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.EBI
J Nat Prod 81: 630-633 (2018)
University of Eastern Piedmont
Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.EBI
J Med Chem 61: 934-945 (2018)
Eli Lilly
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.EBI
Bioorg Med Chem Lett 28: 85-93 (2018)
Bristol-Myers Squibb
Monoterpene indole alkaloid azine derivatives as MDR reversal agents.EBI
Bioorg Med Chem 26: 421-434 (2018)
Universidade De Lisboa
Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation.EBI
Eur J Med Chem 143: 1139-1147 (2018)
The Australian National University
Bioactive products from singlet oxygen photooxygenation of cannabinoids.EBI
Eur J Med Chem 143: 983-996 (2018)
The University of Mississippi
Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents.EBI
Eur J Med Chem 143: 958-969 (2018)
Northwest A&F University
Structure-based identification of a NEDD8-activating enzyme inhibitor via drug repurposing.EBI
Eur J Med Chem 143: 1021-1027 (2018)
University of Macau
Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors.EBI
J Med Chem 61: 1098-1117 (2018)
Takeda Pharmaceutical
Novel sulfenamides and sulfonamides based on pyridazinone and pyridazine scaffolds as CBEBI
Bioorg Med Chem 26: 295-307 (2018)
University of Sassari
Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors.EBI
Bioorg Med Chem 26: 443-454 (2018)
Shanghai Institute of Materia Medica (Simm)
Artocarmins G-M, Prenylated 4-Chromenones from the Stems of Artocarpus rigida and Their Tyrosinase Inhibitory Activities.EBI
J Nat Prod 80: 3172-3178 (2017)
Hiroshima University
Structure-Activity Relationship Studies on a Series of 3?-[Bis(4-fluorophenyl)methoxy]tropanes and 3?-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.EBI
J Med Chem 60: 10172-10187 (2017)
National Institute On Drug Abuse-Intramural Research Program
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.EBI
J Med Chem 61: 119-139 (2018)
University of Ljubljana
Recent encounters with atropisomerism in drug discovery.EBI
NA
Bristol-Myers Squibb Research and Development
Breakthroughs in neuroactive steroid drug discovery.EBI
NA
Sage Therapeutics
Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin.EBI
Eur J Med Chem 143: 854-865 (2018)
University of New Mexico
Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.EBI
Eur J Med Chem 143: 829-842 (2018)
University of Beira Interior
Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.EBI
Eur J Med Chem 143: 792-805 (2018)
Taipei Medical University
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.EBI
Eur J Med Chem 143: 724-731 (2018)
Hefei University of Technology
Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy.EBI
Eur J Med Chem 143: 656-669 (2018)
China Pharmaceutical University
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.EBI
J Med Chem 61: 372-384 (2018)
Universit£
Design, synthesis and evaluation of an anthraquinone derivative conjugated to myelin basic protein immunodominant (MBPEBI
Eur J Med Chem 143: 621-631 (2018)
University of Patras
Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2.EBI
Eur J Med Chem 143: 611-620 (2018)
National Health Research Institutes
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.EBI
J Med Chem 61: 4656-4687 (2018)
China Pharmaceutical University
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinEBI
J Med Chem 61: 650-665 (2018)
Wuxi Apptec
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.EBI
J Med Chem 61: 207-223 (2018)
Janssen Research and Development
Discovery of new GSK-3? inhibitors through structure-based virtual screening.EBI
Bioorg Med Chem Lett 28: 160-166 (2018)
Peking University
Identification of potent lysophosphatidic acid receptor 5 (LPA5) antagonists as potential analgesic agents.EBI
Bioorg Med Chem 26: 257-265 (2018)
Astellas Pharma
Accelerated skin wound healing by selective 11?-Hydroxylase (CYP11B1) inhibitors.EBI
Eur J Med Chem 143: 591-597 (2018)
Saarland University
Xanthine oxidase inhibitory activity of natural and hemisynthetic flavonoids from Gardenia oudiepe (Rubiaceae) inávitro and molecular docking studies.EBI
Eur J Med Chem 143: 577-582 (2018)
Universidad Nacional De C£Rdoba
Structure-activity relationships for inhibitors of Pseudomonas aeruginosa exoenzyme S ADP-ribosyltransferase activity.EBI
Eur J Med Chem 143: 568-576 (2018)
Umea University
Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.EBI
Eur J Med Chem 143: 515-531 (2018)
American University of Ras Al Khaimah
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.EBI
J Med Chem 60: 9885-9904 (2017)
University of Eastern Finland
Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors.EBI
Bioorg Med Chem 26: 245-256 (2018)
Jiangxi Science & Technology Normal University
Synthesis and evaluation of a potent, well-balanced EPEBI
Bioorg Med Chem 26: 200-214 (2018)
Ono Pharmaceutical
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors.EBI
Eur J Med Chem 143: 491-502 (2018)
China Pharmaceutical University
Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts.EBI
Eur J Med Chem 143: 449-463 (2018)
Anhui University of Chinese Medicine
Potent aromatase inhibitors and molecular mechanism of inhibitory action.EBI
Eur J Med Chem 143: 426-437 (2018)
Yunnan University
Design, synthesis and structure-activity relationship of a focused library of ?-phenylalanine derivatives as novel eEF2K inhibitors with apoptosis-inducing mechanisms in breast cancer.EBI
Eur J Med Chem 143: 402-418 (2018)
Sichuan University
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.EBI
Eur J Med Chem 143: 390-401 (2018)
Keimyung University
Discovery of caffeic acid phenethyl ester derivatives as novel myeloid differentiation protein 2 inhibitors for treatment of acute lung injury.EBI
Eur J Med Chem 143: 361-375 (2018)
Wenzhou Medical University
Synthesis and biological characterization of ubenimex-fluorouracil conjugates for anti-cancer therapy.EBI
Eur J Med Chem 143: 334-347 (2018)
Shandong University
Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.EBI
Eur J Med Chem 143: 320-333 (2018)
Beijing University of Chemical Technology
Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.EBI
J Med Chem 60: 10026-10046 (2017)
Chiesi Farmaceutici
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators.EBI
Bioorg Med Chem 26: 266-277 (2018)
Central University of Punjab
Synthesis and anti-influenza virus evaluation of triterpene-sialic acid conjugates.EBI
Bioorg Med Chem 26: 17-24 (2018)
Meiji Pharmaceutical University
Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.EBI
Bioorg Med Chem Lett 28: 145-151 (2018)
Carna Biosciences
Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors.EBI
Bioorg Med Chem Lett 28: 167-169 (2018)
Waseda University
Small molecule inhibitors of anthrax edema factor.EBI
Bioorg Med Chem Lett 28: 134-139 (2018)
Hawaii Biotech
Synthesis and evaluation of biaryl derivatives for structural characterization of selective monoamine oxidase B inhibitors toward Parkinson's disease therapy.EBI
Bioorg Med Chem 26: 232-244 (2018)
Yonsei University
Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases.EBI
Eur J Med Chem 143: 276-282 (2018)
University of Messina
Synthesis and antiproliferative activity of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety.EBI
Eur J Med Chem 143: 266-275 (2018)
Jiangxi Science & Technology Normal University
7-Methylguanosine monophosphate analogues with 5'-(1,2,3-triazoyl) moiety: Synthesis and evaluation as the inhibitors of cNIIIB nucleotidase.EBI
Bioorg Med Chem 26: 191-199 (2018)
University of Warsaw
Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction.EBI
Bioorg Med Chem 26: 215-224 (2018)
Panjab University
Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2.EBI
J Med Chem 60: 10231-10244 (2017)
Shanghaitech University
Synthesis of radioiodinated probes targeted toward matrix metalloproteinase-12.EBI
Bioorg Med Chem Lett 28: 193-195 (2018)
Kobe Pharmaceutical University
Structure-based design, synthesis, and binding mode analysis of novel and potent chymase inhibitors.EBI
Bioorg Med Chem Lett 28: 188-192 (2018)
Asubio Pharma
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.EBI
Bioorg Med Chem 26: 141-151 (2018)
Poznan University of Medical Sciences
Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity.EBI
J Med Chem 60: 10188-10204 (2017)
Martin-Luther University of Halle-Wittenberg
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.EBI
J Med Chem 61: 265-285 (2018)
Shenyang Pharmaceutical University
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.EBI
J Med Chem 61: 140-157 (2018)
China Pharmaceutical University
4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice.EBI
J Med Chem 60: 10245-10256 (2017)
University of Cape Town
Bisindolylmethane thiosemicarbazides as potential inhibitors of urease: Synthesis and molecular modeling studies.EBI
Bioorg Med Chem 26: 152-160 (2018)
Imam Abdulrahman Bin Faisal University
Highly Selective and Potent?4?2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.EBI
J Med Chem 60: 10092-10104 (2017)
Torrey Pines Institute For Molecular Studies
Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors.EBI
Eur J Med Chem 143: 182-199 (2018)
Southern Medical University
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.EBI
Eur J Med Chem 143: 123-136 (2018)
Shenyang Pharmaceutical University
Discovery of novel purine nucleoside derivatives as phosphodiesterase 2 (PDE2) inhibitors: Structure-based virtual screening, optimization and biological evaluation.EBI
Bioorg Med Chem 26: 119-133 (2018)
East China University of Science and Technology
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.EBI
Bioorg Med Chem Lett 28: 31-34 (2018)
Sanford Burnham Prebys Medical Discovery Institute
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-? production.EBI
Bioorg Med Chem Lett 28: 24-30 (2018)
Padmashri Vikhe Patil College of Arts
Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.EBI
J Med Chem 60: 9990-10012 (2017)
Sichuan University
Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.EBI
J Med Chem 60: 9531-9544 (2017)
University of Catania
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88EBI
J Med Chem 60: 10071-10091 (2017)
Astrazeneca
Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.EBI
Eur J Med Chem 143: 33-47 (2018)
East China University of Science and Technology
Chemical probes and inhibitors of bromodomains outside the BET family.EBI
Medchemcomm 7: 2246-2264 (2016)
University of Oxford
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.EBI
Bioorg Med Chem 26: 25-36 (2018)
St. Jude Children'S Research Hospital
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.EBI
Bioorg Med Chem Lett 28: 15-23 (2018)
Wuxi Apptec
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.EBI
J Med Chem 60: 10056-10070 (2017)
Genentech
Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.EBI
Bioorg Med Chem Lett 28: 49-52 (2018)
Renmin Hospital of Wuhan University
The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease.EBI
Bioorg Med Chem Lett 28: 43-48 (2018)
Bristol-Myers Squibb
A novel series of enoyl reductase inhibitors targeting the ESKAPE pathogens, Staphylococcus aureus and Acinetobacter baumannii.EBI
Bioorg Med Chem 26: 65-76 (2018)
Novalex Therapeutics
Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a?-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease.EBI
J Med Chem 61: 396-402 (2018)
Medifron Dbt
New Caspase-1 inhibitor by scaffold hopping into bio-inspired 3D-fragment space.EBI
Bioorg Med Chem Lett 27: 5373-5377 (2017)
Edelris
Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2.EBI
Bioorg Med Chem Lett 27: 5404-5408 (2017)
Guizhou Medical University
Recent advances in the discovery of small molecule c-Met Kinase inhibitors.EBI
NA
Nirma University
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.EBI
J Med Chem 60: 9676-9690 (2017)
Merck
Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment.EBI
J Med Chem 60: 10205-10219 (2017)
Chinese Academy of Sciences
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.EBI
J Med Chem 60: 10151-10171 (2017)
Genentech
Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.EBI
J Med Chem 60: 10013-10025 (2017)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)
Structure-activity relationships and docking studies of synthetic 2-arylindole derivatives determined with aromatase and quinone reductase 1.EBI
Bioorg Med Chem Lett 27: 5393-5399 (2017)
University of Hawai'I At Hilo
Discovery and in vivo effects of novel human natriuretic peptide receptor A (NPR-A) agonists with improved activity for rat NPR-A.EBI
Bioorg Med Chem 25: 6680-6694 (2017)
Asubio Pharma
Optimization of peptide-based polyagonists for treatment of diabetes and obesity.EBI
Bioorg Med Chem 26: 2873-2881 (2018)
Novo Nordisk Research Center Indianapolis
Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [EBI
Bioorg Med Chem Lett 27: 5467-5472 (2017)
University of Kentucky
Benzoxaboroles as Efficient Inhibitors of the ?-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.EBI
ACS Med Chem Lett 8: 1194-1198 (2017)
University of Montpellier
Discovery of Thiophene[3,2-EBI
ACS Med Chem Lett 8: 1188-1193 (2017)
Shandong University
?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.EBI
ACS Med Chem Lett 8: 1177-1182 (2017)
Vrije Universiteit Brussel
Structure-Based Design and Synthesis of New Estrane-Pyridine Derivatives as Cytochrome P450 (CYP) 1B1 Inhibitors.EBI
ACS Med Chem Lett 8: 1159-1164 (2017)
Chu De Qu£Bec-Research Center
Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8.EBI
ACS Med Chem Lett 8: 1148-1152 (2017)
University of Minnesota
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.EBI
ACS Med Chem Lett 8: 1142-1147 (2017)
Shenyang Pharmaceutical University
Structure-Based Discovery of Thiosemicarbazone Metalloproteinase Inhibitors for Hemorrhage Treatment in Snakebites.EBI
ACS Med Chem Lett 8: 1136-1141 (2017)
Instituto De Ci£Ncias Exatas
Lysine-Specific Demethylase 1 (LSD1) Inhibitors as Potential Treatment for Different Types of Cancers.EBI
ACS Med Chem Lett 8: 1134-1135 (2017)
Therachem Research Medilab (India)
Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases.EBI
ACS Med Chem Lett 8: 1132-1133 (2017)
Therachem Research Medilab (India)
Selective Estrogen Receptor Degraders (SERDs): A Promising Treatment to Overcome Resistance to Endocrine Therapy in ER?-Positive Breast Cancer.EBI
ACS Med Chem Lett 8: 1129-1131 (2017)
Therachem Research Medilab (India)
Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme.EBI
Bioorg Med Chem Lett 27: 5400-5403 (2017)
Csir-Indian Institute of Integrative Medicine
Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors.EBI
Bioorg Med Chem Lett 27: 5473-5480 (2017)
Brigham Young University
Identification of pyruvate dehydrogenase kinase 1 inhibitors with anti-osteosarcoma activity.EBI
Bioorg Med Chem Lett 27: 5450-5453 (2017)
Sichuan University
Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.EBI
Eur J Med Chem 143: 2005-2014 (2018)
Universit£
A routinely used protein staining dye acts as an inhibitor of wild type and mutant alpha-synuclein aggregation and modulator of neurotoxicity.EBI
Eur J Med Chem 143: 1174-1184 (2018)
National Institute of Immunology
Anti-amyloidogenic and anti-apoptotic effect of ?-bisabolol against A? induced neurotoxicity in PC12 cells.EBI
Eur J Med Chem 143: 1196-1207 (2018)
Alagappa University
The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.EBI
Eur J Med Chem 143: 1790-1806 (2018)
Wayne State University
Unique arginine array improves cytosolic localization of hydrocarbon-stapled peptides.EBI
Bioorg Med Chem 26: 1197-1202 (2018)
Yale University
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).EBI
J Med Chem 60: 9960-9973 (2017)
Genomics Institute of The Novartis Research Foundation
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.EBI
J Med Chem 60: 9860-9873 (2017)
Pfizer
Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.EBI
J Med Chem 61: 1425-1435 (2018)
Galapagos
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.EBI
J Med Chem 60: 10118-10134 (2017)
University of Cape Town
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.EBI
Bioorg Med Chem Lett 27: 5415-5419 (2017)
Roche Pharma Research and Early Development
Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors.EBI
Bioorg Med Chem 25: 6674-6679 (2017)
China Pharmaceutical University
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.EBI
Eur J Med Chem 143: 1847-1857 (2018)
The First Affiliated Hospital of Dalian Medical University
Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies.EBI
Eur J Med Chem 143: 1931-1941 (2018)
Medical University of Gdansk
Oxyprenylated Phenylpropanoids Bind to MT1 Melatonin Receptors and Inhibit Breast Cancer Cell Proliferation and Migration.EBI
J Nat Prod 80: 3324-3329 (2017)
Duquesne University
Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?EBI
J Med Chem 61: 444-452 (2018)
Benevolentbio
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.EBI
J Med Chem 60: 9470-9489 (2017)
Csir-Indian Institute of Integrative Medicine
Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors.EBI
Bioorg Med Chem Lett 27: 5429-5435 (2017)
Shanghai Institute of Technology
Cornusides A-O, Bioactive Iridoid Glucoside Dimers from the Fruit of Cornus officinalis.EBI
J Nat Prod 80: 3103-3111 (2017)
Beijing University of Chinese Medicine
Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HTEBI
Bioorg Med Chem Lett 27: 5420-5423 (2017)
Shanghai Institute of Pharmaceutical Industry
(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.EBI
Bioorg Med Chem Lett 27: 5409-5414 (2017)
De Montfort University
Functionalized 2,1-benzothiazine 2,2-dioxides as new inhibitors of Dengue NS5 RNA-dependent RNA polymerase.EBI
Eur J Med Chem 143: 1667-1676 (2018)
Universit£
Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors.EBI
Eur J Med Chem 143: 1604-1615 (2018)
Srinakharinwirot University
Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.EBI
J Med Chem 61: 4290-4300 (2018)
Wenzhou Medical University
Natural Products with Heteroatom-Rich Ring Systems.EBI
J Nat Prod 80: 3060-3079 (2017)
University of Auckland
Recent advances in the discovery of potent and selective HDAC6 inhibitors.EBI
Eur J Med Chem 143: 1406-1418 (2018)
Shandong University
Recent advances in the search for novel 5-lipoxygenase inhibitors for the treatment of asthma.EBI
Eur J Med Chem 153: 65-7