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Decoding the Papain Inhibitor from 
J Nat Prod 83: 2983-2995 (2020)
University Of Applied Sciences Of Darmstadt
Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
Eur J Med Chem 208: (2020)
Qilu University Of Technology (Shandong Academy Of Sciences)
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
J Med Chem 63: 12748-12772 (2020)
Chinese Academy Of Sciences
Rapid Solid-Phase Construction of Serine Hydrolase Probes Results in Selective Activity-Based Probes for Acyl Protein Thioesterases-1/2.
J Med Chem 63: 11845-11853 (2020)
Ku Leuven
Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from
J Nat Prod 83: 2950-2959 (2020)
Sichuan University
Discovery of novel quinazoline derivatives as potent PI3K? inhibitors with high selectivity.
Eur J Med Chem 208: (2020)
China Pharmaceutical University
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.
Eur J Med Chem 208: (2020)
Shanghai Jiao Tong University
Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor.
Bioorg Med Chem Lett 30: (2020)
Cadila Healthcare
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Bioorg Med Chem Lett 30: (2020)
Merck
A guanidinium-based inhibitor of a type I isopentenyl diphosphate isomerase.
Bioorg Med Chem Lett 30: (2020)
University Of British Columbia
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.
J Med Chem 63: 11045-11053 (2020)
Philipps-University
Synthesis, biological evaluation, in silico modeling and crystallization of novel small monocationic molecules with potent antiproliferative activity by dual mechanism.
Eur J Med Chem 207: (2020)
Campus Cartuja S/N. University Of Granada
Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D
Bioorg Med Chem Lett 30: (2020)
Sumitomo Dainippon Pharma.
Natural and Semisynthetic Chalcones as Dual FLT3 and Microtubule Polymerization Inhibitors.
J Nat Prod 83: 3111-3121 (2020)
Lahore University Of Management Sciences
Targeting the aryl hydrocarbon receptor with a novel set of triarylmethanes.
Eur J Med Chem 207: (2020)
Universitat De Val£Ncia. Av. Vicente Andr£S Estell£S
Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
Eur J Med Chem 208: (2020)
University Of Groningen
Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays.
Eur J Med Chem 208: (2020)
University Of Genoa
Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).
J Med Chem 63: 11639-11662 (2020)
Bayer
Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
Eur J Med Chem 206: (2020)
Sun Yat-Sen University
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.
Eur J Med Chem 207: (2020)
Korea Institute Of Science And Technology (Kist)
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
Eur J Med Chem 208: (2020)
Southern Medical University
Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer.
Eur J Med Chem 208: (2020)
Shenyang Pharmaceutical University
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
J Med Chem 63: 11854-11881 (2020)
Bayer
Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors.
Bioorg Med Chem Lett 30: (2020)
Nodthera
Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-?B Ligand with a Superior Therapeutic Index.
J Med Chem 63: 12043-12059 (2020)
Agricultural University Of Athens
Bioactivity-Guided Discovery of Human Carboxylesterase Inhibitors from the Roots of
J Nat Prod 83: 2940-2949 (2020)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
Eur J Med Chem 207: (2020)
China Pharmaceutical University
A dual-acting 5-HT
Eur J Med Chem 208: (2020)
Jagiellonian University Medical College
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Eur J Med Chem 207: (2020)
Chinese Academy Of Sciences
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
Eur J Med Chem 205: (2020)
Southern Medical University
Design, synthesis and biological evaluation of novel heptamethine cyanine dye-erlotinib conjugates as antitumor agents.
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
Eur J Med Chem 208: (2020)
National Institute On Drug Abuse - Intramural Research Program
Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity.
Eur J Med Chem 208: (2020)
Cairo University
First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters.
J Med Chem 63: 11548-11572 (2020)
Fraunhofer Ime
Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1
J Med Chem 63: 11169-11194 (2020)
D3-Pharmachemistry
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia.
ACS Med Chem Lett 11: 1678-1687 (2020)
Convergence Pharmaceuticals
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu
ACS Med Chem Lett 11: 1773-1779 (2020)
Vanderbilt University
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
ACS Med Chem Lett 11: 1759-1765 (2020)
Stanford University School Of Medicine
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9).
ACS Med Chem Lett 11: 1751-1758 (2020)
Princ
Facile Synthesis of Aminomethyl Phosphinate Esters as Serine Protease Inhibitors with Primed Site Interaction.
ACS Med Chem Lett 11: 1739-1744 (2020)
Ku Leuven
Insights into the Molecular Determinants Involved in Urocontrin and Urocontrin A Action.
ACS Med Chem Lett 11: 1717-1722 (2020)
Universit£
A Phosphoramidate Strategy Enables Membrane Permeability of a Non-nucleotide Inhibitor of the Prolyl Isomerase Pin1.
ACS Med Chem Lett 11: 1704-1710 (2020)
University Of California San Francisco
Identification of Novel Rho-Kinase-II Inhibitors with Vasodilatory Activity.
ACS Med Chem Lett 11: 1694-1703 (2020)
Banasthali Vidyapith
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).
ACS Med Chem Lett 11: 1688-1693 (2020)
Merck
Novel 4-Heteroarylcarbonyl-N-(phenyl or heteroaryl) Piperidine-1-carboxamides as Tankyrase Inhibitors.
ACS Med Chem Lett 11: 1676-1677 (2020)
Lauren Mccallister
Novel Heteroaromatic Compounds as Vanin Inhibitors.
ACS Med Chem Lett 11: 1674-1675 (2020)
Lauren Mccallister
Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders.
ACS Med Chem Lett 11: 1671-1673 (2020)
Lauren Mccallister
2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAF
Eur J Med Chem 208: (2020)
Korea Institute Of Science And Technology (Kist)
Design, synthesis and molecular docking study of ?-triazolylsialosides as non-hydrolyzable and potent CD22 ligands.
Eur J Med Chem 208: (2020)
Academia Sinica
The components and activities analysis of a novel anticoagulant candidate dHG-5.
Eur J Med Chem 207: (2020)
University Of Chinese Academy Of Sciences
Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase.
Eur J Med Chem 207: (2020)
Csir-India
The synthesis and anti-tumour properties of novel 4-substituted phthalazinones as Aurora B kinase inhibitors.
Bioorg Med Chem Lett 30: (2020)
Lanzhou University
Lycosquarrines A-R,
J Nat Prod 83: 2831-2843 (2020)
China Pharmaceutical University
7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor.
J Med Chem 63: 11920-11933 (2020)
University Of Groningen
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
J Med Chem 63: 12116-12127 (2020)
The University Of Sydney
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs.
ACS Med Chem Lett 11: 1732-1738 (2020)
University Of California Santa Cruz
4-Amino-1,2,4-triazole-3-thione-derived Schiff bases as metallo-?-lactamase inhibitors.
Eur J Med Chem 208: (2020)
Universit£
Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint.
J Med Chem 63: 11271-11285 (2020)
Jagiellonian University
Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.
bioRxiv (2020)
Pfizer
Mycophenolic anilides as broad specificity inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors.
Bioorg Med Chem Lett 30: (2020)
University Of Houston
Structural basis for producing selective MAP2K7 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Osaka Prefecture University
Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists.
Bioorg Med Chem Lett 30: (2020)
Seoul National University
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
J Med Chem 63: 11725-11755 (2020)
Tu Dortmund University
Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective.
J Med Chem 63: 14197-14215 (2020)
Key Laboratory Of Henan Provinc
Aryloxy Diester Phosphonamidate Prodrugs of Phosphoantigens (ProPAgens) as Potent Activators of V?9/V?2 T-Cell Immune Responses.
J Med Chem 63: 11258-11270 (2020)
Cardiff University
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
J Med Chem 63: 12542-12573 (2020)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
Eur J Med Chem 206: (2020)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Merck
Directing Drugs to Bugs: Antibiotic-Carbohydrate Conjugates Targeting Biofilm-Associated Lectins of
J Med Chem 63: 11707-11724 (2020)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers.
J Med Chem 63: 11012-11033 (2020)
West China Hospital Of Sichuan University
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.
Eur J Med Chem 207: (2020)
Faculty Of Science And The University Of Sydney
Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy.
Eur J Med Chem 207: (2020)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Structure-activity relationships of GPX4 inhibitor warheads.
Bioorg Med Chem Lett 30: (2020)
Institute Of Mit And Harvard
Structure-activity relationship study of tryptophan-based butyrylcholinesterase inhibitors.
Eur J Med Chem 208: (2020)
University Of Ljubljana
Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.
Eur J Med Chem 206: (2020)
Washington University School Of Medicine
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
Bioorg Med Chem Lett 30: (2020)
Hanoi University Of Pharmacy
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
J Med Chem 63: 14357-14381 (2020)
Genentech
Repurposing of Drugs-The Ketamine Story.
J Med Chem 63: 13514-13525 (2020)
University Of Houston
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.
J Med Chem 63: 14228-14242 (2020)
University Of Toyama
New cannabinoid receptor antagonists as pharmacological tool.
Bioorg Med Chem 28: (2020)
Instituto De Qu£Mica M£Dica (Csic)
Synthesis and evaluation of 17?-triazolyl and 9?-cyano derivatives of estradiol.
Bioorg Med Chem 28: (2020)
Marquette University
Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors.
Bioorg Med Chem 28: (2020)
Yantai University
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.
Bioorg Med Chem 28: (2020)
Jiangxi Science & Technology Normal University
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR
Bioorg Med Chem 28: (2020)
Zhejiang University
SAR study of bisamides as cyclophilin a inhibitors for the development of host-targeting therapy for hepatitis C virus infection.
Bioorg Med Chem 28: (2020)
Chonnam National University
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors.
Bioorg Med Chem 28: (2020)
Takeda Pharmaceuticals International
New drug approvals for 2019: Synthesis and clinical applications.
Eur J Med Chem 205: (2020)
Zhengzhou University
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
J Med Chem 63: 14530-14559 (2020)
Astrazeneca
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
J Med Chem 63: 13578-13594 (2020)
TBA
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose.
J Med Chem 63: 13546-13560 (2020)
Pfizer
Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket.
J Med Chem 63: 11972-11989 (2020)
Max Planck Institute Of Molecular Physiology
Anti-glioma effects of 2-aminothiophene-3-carboxamide derivatives, ANO1 channel blockers.
Eur J Med Chem 208: (2020)
Korea University
Discovery of 9-Cyclopropylethynyl-2-((
J Med Chem 63: 13526-13545 (2020)
Galapagos
Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.
J Med Chem 63: 11149-11168 (2020)
China Pharmaceutical University
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
J Med Chem 63: 10984-11011 (2020)
National Institutes Of Health
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
J Med Chem 63: 12929-12941 (2020)
Vrije Universiteit Brussel
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NH
J Med Chem 63: 10782-10795 (2020)
University Of Ferrara
Design and Identification of a GPR40 Full Agonist (
J Med Chem 63: 10352-10379 (2020)
Takeda Pharmaceutical
Structure-activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy.
Eur J Med Chem 208: (2020)
Central China Normal University
Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents.
Eur J Med Chem 208: (2020)
Soochow University
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Jiangnan University
Discovery of ONO-8590580: A novel, potent and selective GABA
Bioorg Med Chem Lett 30: (2020)
Charles River Discovery Research Services
Fragment-based lead discovery of a novel class of small molecule antagonists of neuropeptide B/W receptor subtype 1 (GPR7).
Bioorg Med Chem Lett 30: (2020)
Merck
Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3K? and mTOR Kinases for the Treatment of Solid Tumors.
J Med Chem 63: 11121-11130 (2020)
Sphaera Pharma
Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
J Med Chem 63: 10829-10854 (2020)
Shandong University
Synthesis and Evaluation of 4-Hydroxycoumarin Imines as Inhibitors of Class II Myosins.
J Med Chem 63: 11131-11148 (2020)
University Of Nevada
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.
Bioorg Med Chem Lett 30: (2020)
Sichuan University
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb
Synthesis and SAR of a series of mGlu
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase.
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb Research And Development
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
J Med Chem 63: 11085-11099 (2020)
University Of Illinois At Chicago
DPAGT1 Inhibitors of Capuramycin Analogues and Their Antimigratory Activities of Solid Tumors.
J Med Chem 63: 10855-10878 (2020)
University Of Tennessee Health Science Center
Catch and Anchor Approach To Combat Both Toxicity and Longevity of Botulinum Toxin A.
J Med Chem 63: 11100-11120 (2020)
Boston University School Of Medicine
Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor ? (PPAR?).
J Med Chem 63: 10908-10920 (2020)
New York University
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.
Eur J Med Chem 208: (2020)
Lanzhou University
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
Eur J Med Chem 208: (2020)
Sapienza Universit£
Factor XII/XIIa inhibitors: Their discovery, development, and potential indications.
Eur J Med Chem 208: (2020)
University Of Namur
Synthesis of biphenyl oxazole derivatives via Suzuki coupling and biological evaluations as nucleotide pyrophosphatase/phosphodiesterase-1 and -3 inhibitors.
Eur J Med Chem 208: (2020)
Quaid-I-Azam University
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.
Eur J Med Chem 208: (2020)
Goethe University Frankfurt
Discovery of Novel pERK1/2- or ?-Arrestin-Preferring 5-HT
J Med Chem 63: 10946-10971 (2020)
Jagiellonian University Medical College
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.
Eur J Med Chem 207: (2020)
Xiamen University
Rational design of new multitarget histamine H
Eur J Med Chem 207: (2020)
Jagiellonian University Medical College
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as ?7 nicotinic receptor antagonists.
Eur J Med Chem 207: (2020)
Peking University
7-Azaindolequinuclidinones (7-AIQD): A novel class of cannabinoid 1 (CB1) and cannabinoid 2 (CB2) receptor ligands.
Bioorg Med Chem Lett 30: (2020)
University Of Arkansas For Medical Sciences
Tricyclic sulfones as potent, selective and efficacious ROR?t inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.
Bioorg Med Chem Lett 30: (2020)
Chinese Academy Of Sciences
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold.
J Med Chem 63: 10796-10815 (2020)
Univ Montpellier
Bifunctional and Unusual Amino Acid ?- or ?-Ester Prodrugs of Nucleoside Analogues for Improved Affinity to ATB
J Med Chem 63: 10816-10828 (2020)
Jiangxi University Of Traditional Chinese Medicine
Highly Selective Sub-Nanomolar Cathepsin S Inhibitors by Merging Fragment Binders with Nitrile Inhibitors.
J Med Chem 63: 11801-11808 (2020)
Grunenthal
Cannabitwinol, a Dimeric Phytocannabinoid from Hemp,
J Nat Prod 83: 2727-2736 (2020)
University Of Naples Federico Ii
Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities.
J Med Chem 63: 11054-11084 (2020)
Albany College Of Pharmacy And Health Sciences
Isoquinolinone derivatives as potent CNS multi-receptor D
Eur J Med Chem 207: (2020)
Jiangsu Ocean University
3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies.
Eur J Med Chem 207: (2020)
Jouf University
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Discovery of an Inhibitor for the TREK-1 Channel Targeting an Intermediate Transition State of Channel Gating.
J Med Chem 63: 10972-10983 (2020)
Shanghai Institute Of Materia Medica
N-terminal modified cyclopeptidic mimetics of Apollo
Bioorg Med Chem Lett 30: 127401 (2020)
China Pharmaceutical University
Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and trytophan 2,3-dioxygenase (TDO).
Eur J Med Chem 207: (2020)
Sichuan University
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from
J Nat Prod 84: 713-723 (2021)
Universidad Nacional Aut£Noma De M£Xico
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
J Med Chem 63: 14243-14275 (2020)
Endotherm
Anti-
J Med Chem 63: 13330-13354 (2020)
Commonwealth Scientific And Industrial Research Organization
Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions.
Eur J Med Chem 207: (2020)
China Pharmaceutical University
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.
J Med Chem 63: 13228-13257 (2020)
China Pharmaceutical University
Bioinspired Hybrid Fluorescent Ligands for the FK1 Domain of FKBP52.
J Med Chem 63: 10330-10338 (2020)
Universit£
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
J Med Chem 63: 10433-10459 (2020)
Oric Pharmaceuticals
Discovery of Potent and Selective PI3K? Inhibitors.
J Med Chem 63: 11235-11257 (2020)
Arcus Biosciences
Discovery of the first potent and selective ?
Eur J Med Chem 208: (2020)
University Of Strathclyde
Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies.
Eur J Med Chem 206: (2020)
Ciudad Universitaria
Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
Eur J Med Chem 206: (2020)
Ludwig-Maximilians University
Half-life extension of peptidic APJ agonists by N-terminal lipid conjugation.
Bioorg Med Chem Lett 30: 127499 (2020)
Amgen
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
J Med Chem 63: 9856-9875 (2020)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors.
Bioorg Med Chem Lett 30: 127508 (2020)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Structure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT
Bioorg Med Chem Lett 30: 127511 (2020)
Kalamazoo College
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.
Med Res Rev (2020)
University Of Bonn
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.
J Med Chem 63: 10396-10411 (2020)
Gifu Pharmaceutical University
Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities.
Eur J Med Chem 203: (2020)
China Pharmaceutical University
Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists.
J Med Chem 63: 13466-13513 (2020)
University Of Siena
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
J Med Chem 63: 13205-13227 (2020)
South China Agricultural University
Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity.
J Med Chem 63: 9660-9671 (2020)
The Scripps Research Institute
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.
J Med Chem 63: 11286-11301 (2020)
Sun Yat-Sen University
Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
Eur J Med Chem 205: (2020)
Ku Leuven
Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells.
ACS Med Chem Lett 11: 1627-1633 (2020)
Universidad Nacional Aut£Noma De M£Xico
Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.
ACS Med Chem Lett 11: 1620-1626 (2020)
University Of Sussex
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
ACS Med Chem Lett 11: 1588-1597 (2020)
Genentech
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
ACS Med Chem Lett 11: 1581-1587 (2020)
Glaxosmithkline Medicines Research Centre
Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers.
ACS Med Chem Lett 11: 1573-1580 (2020)
University Of Zurich
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.
ACS Med Chem Lett 11: 1567-1572 (2020)
Jinan University
Virtual Screening for Ligand Discovery at the ?
ACS Med Chem Lett 11: 1555-1561 (2020)
Harvard Medical School
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
ACS Med Chem Lett 11: 1548-1554 (2020)
Merck
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition.
ACS Med Chem Lett 11: 1535-1538 (2020)
The University Of Notre Dame
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B
ACS Med Chem Lett 11: 1529-1534 (2020)
Incerebro
Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines.
J Med Chem 63: 10263-10286 (2020)
University Of Michigan
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.
Eur J Med Chem 204: (2020)
University Of Michigan
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
Bioorg Med Chem Lett 30: (2020)
Jiangsu Ocean University
Biological evaluation and SAR analysis of novel covalent inhibitors against fructose-1,6-bisphosphatase.
Bioorg Med Chem 28: (2020)
Anhui University Of Technology
Synthesis and activity of isoleucine sulfonamide derivatives as novel botulinum neurotoxin serotype A light chain inhibitors.
Bioorg Med Chem 28: (2020)
California State University
Boronic acid-based arginase inhibitors in cancer immunotherapy.
Bioorg Med Chem 28: (2020)
Oncoarendi Therapeutics
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
Bioorg Med Chem 28: (2020)
National Research Centre
The neuronal calcium ion channel activity of constrained analogues of MONIRO-1.
Bioorg Med Chem 28: (2020)
The University Of Queensland
Identification of the first noncompetitive SARM1 inhibitors.
Bioorg Med Chem 28: (2020)
Umass Medical School
Suramin derivatives play an important role in blocking the interaction between FGF1 and FGFRD2 to inhibit cell proliferation.
Eur J Med Chem 206: (2020)
National Tsing Hua University
Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation.
Eur J Med Chem 206: (2020)
University Of Arkansas For Medical Sciences
From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators.
Eur J Med Chem 206: (2020)
University Of Wisconsin-Madison
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
Eur J Med Chem 206: (2020)
Nankai University
Synthesis and in vitro evaluation of vanillin derivatives as multi-target therapeutics for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 30: 127505 (2020)
Robert Gordon University
Discovery of
J Med Chem 63: 10307-10329 (2020)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Isolation, reactivity, pharmacological activities and total synthesis of hispanolone and structurally related diterpenes from Labiatae plants.
Bioorg Med Chem Lett 30: (2020)
Csic
Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of
J Med Chem 63: 10380-10395 (2020)
Janssen Biopharma
Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.
J Med Chem 63: 10246-10262 (2020)
The George Washington University
Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT
J Med Chem 63: 9928-9949 (2020)
University Of Copenhagen
Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma.
Eur J Med Chem 206: (2020)
Xiamen University
Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.
Eur J Med Chem 205: (2020)
University Of Milan
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.
J Med Chem 63: 10879-10896 (2020)
Pfizer
Rational Design and Synthesis of Methyl-?-d-galactomalonyl Phenyl Esters as Potent Galectin-8
J Med Chem 63: 11573-11584 (2020)
Griffith University
Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist.
Bioorg Med Chem Lett 30: 127496 (2020)
Crinetics Pharmaceuticals
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.
Bioorg Med Chem Lett 30: 127474 (2020)
Bristol Myers Squibb
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.
J Med Chem 63: 13291-13315 (2020)
St. John'S University
The Essential Medicinal Chemistry of Cannabidiol (CBD).
J Med Chem 63: 12137-12155 (2020)
University Of Minnesota
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.
J Med Chem 63: 10460-10473 (2020)
Astrazeneca
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
J Med Chem 63: 10339-10351 (2020)
Leipzig University
Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.
bioRxiv (2020)
National Institutes Of Health
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
Bioorg Med Chem Lett 30: (2020)
Concept Life Sciences
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Bioorg Med Chem Lett 30: 127493 (2020)
Polish Academy Of Sciences
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Bioorg Med Chem Lett 30: 127495 (2020)
Bristol Myers Squibb
Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.
J Med Chem 63: 9154-9167 (2020)
Guangxi Normal University
Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket.
J Med Chem 63: 9828-9837 (2020)
Sun Yat-Sen University
Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
Eur J Med Chem 205: (2020)
Shenzhen Technology University
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
J Med Chem 63: 9020-9044 (2020)
Gsk
Discovery of Clinical Candidate (5-(3-(4-Chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an Orally Bioavailable Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.
J Med Chem 63: 10045-10060 (2020)
China Pharmaceutical University
MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis.
J Med Chem 63: 9695-9704 (2020)
Stanford University School Of Medicine
Exploration of Alternative Scaffolds for P2Y
J Med Chem 63: 9563-9589 (2020)
National Institute Of Diabetes And Digestive And Kidney Diseases
Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant
J Med Chem 63: 9540-9562 (2020)
Purdue University
Structure-Activity Relationship Studies of ?-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family.
J Med Chem 63: 9340-9359 (2020)
Leiden University & Oncode Institute
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.
J Med Chem 63: 10030-10044 (2020)
China Pharmaceutical University
Non-naturally Occurring Regio Isomer of Lysophosphatidylserine Exhibits Potent Agonistic Activity toward G Protein-Coupled Receptors.
J Med Chem 63: 9990-10029 (2020)
The University Of Tokyo
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
J Med Chem 63: 9888-9911 (2020)
University Of Texas Md Anderson Cancer Center
Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.
J Med Chem 63: 9672-9694 (2020)
University Of Salerno
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity.
J Med Chem 63: 9464-9483 (2020)
University College London
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-
J Med Chem 63: 9181-9196 (2020)
Janssen Research & Development
Advances in the Design of Genuine Human Tyrosinase Inhibitors for Targeting Melanogenesis and Related Pigmentations.
J Med Chem 63: 13428-13443 (2020)
Universit£
Superior Pyrimidine Derivatives as Selective ABCG2 Inhibitors and Broad-Spectrum ABCB1, ABCC1, and ABCG2 Antagonists.
J Med Chem 63: 10412-10432 (2020)
Rheinische Friedrich-Wilhelms-University Bonn
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
J Med Chem 63: 13561-13577 (2020)
Pfizer
Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase.
J Med Chem 63: 9773-9786 (2020)
Ut Southwestern Medical Center
Structural Analysis of VDR Complex with ZK168281 Antagonist.
J Med Chem 63: 9457-9463 (2020)
Institut De G£N£Tique Et De Biologie Mol£Culaire Et Cellulaire (Igbmc)
Highly Potent and Selective
J Med Chem 63: 9212-9227 (2020)
Purdue University
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors:
J Med Chem 63: 9237-9257 (2020)
Universitat De Barcelona
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
J Med Chem 63: 10061-10085 (2020)
Ontario Institute For Cancer Research
Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders.
J Med Chem 63: 9977-9989 (2020)
Icahn School Of Medicine At Mount Sinai
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
J Med Chem 63: 9787-9802 (2020)
Chinese Academy Of Sciences
Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity.
J Med Chem 63: 10474-10495 (2020)
Sichuan University
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
J Med Chem 63: 10224-10234 (2020)
Goethe-University Frankfurt
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
J Med Chem 63: 9705-9730 (2020)
Astrazeneca
Usnic Acid Conjugates with Monoterpenoids as Potent Tyrosyl-DNA Phosphodiesterase 1 Inhibitors.
J Nat Prod 83: 2320-2329 (2020)
TBA
Allicin, a Potent New Ornithine Decarboxylase Inhibitor in Neuroblastoma Cells.
J Nat Prod 83: 2518-2527 (2020)
Michigan State University
Targeting Protein Folding: A Novel Approach for the Treatment of Pathogenic Bacteria.
J Med Chem 63: 13355-13388 (2020)
University Of W£Rzburg
Targeting Metabolism of Extracellular Nucleotides via Inhibition of Ectonucleotidases CD73 and CD39.
J Med Chem 63: 13444-13465 (2020)
Arcus Biosciences
Generation of Leads for ?-Secretase Modulation.
J Med Chem 63: 8216-8230 (2020)
Merck
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
J Med Chem 63: 8276-8295 (2020)
Genomics Institute Of The Novartis Research Foundation
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3K? inhibitors.
Bioorg Med Chem Lett 30: (2020)
Southwest Jiaotong University
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 30: (2020)
Janssen Pharmaceutical Companies Of Johnson & Johnson
Synthesis and biological evaluation of thiazole derivatives on basic defects underlying cystic fibrosis.
Bioorg Med Chem Lett 30: 127473 (2020)
Rccs Istituto Giannina Gaslini
Discovery of noscapine derivatives as potential ?-tubulin inhibitors.
Bioorg Med Chem Lett 30: 127489 (2020)
Shahid Beheshti University
New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation.
Bioorg Med Chem Lett 30: (2020)
Guru Nanak Dev University
Discovery of USP7 small-molecule allosteric inhibitors.
Bioorg Med Chem Lett 30: (2020)
Medivir
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines.
Bioorg Med Chem Lett 30: (2020)
Daiichi Sankyo
Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.
Bioorg Med Chem Lett 30: (2020)
University Of Science & Technology (Ust)
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
Bioorg Med Chem 28: (2020)
East China Normal University
An investigative study of antitumor properties of a novel thiazolo[4,5-d]pyrimidine small molecule revealing superior antitumor activity with CDK1 selectivity and potent pro-apoptotic properties.
Bioorg Med Chem 28: (2020)
Egyptian Russian University
The design, synthesis and evaluation of 2-aminobenzoxazole analogues as potent and orally efficacious ChemR23 inhibitors.
Bioorg Med Chem 28: (2020)
Kyowa Kirin
Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.
Eur J Med Chem 205: (2020)
Soochow University
Discovery of a d-pro-lys peptidomimetic inhibitor of MMP9: Addressing the gelatinase selectivity beyond S1' subsite.
Bioorg Med Chem Lett 30: 127467 (2020)
University Of Florence
Integrating DNA-encoded chemical libraries with virtual combinatorial library screening: Optimizing a PARP10 inhibitor.
Bioorg Med Chem Lett 30: (2020)
Mcdaniel College
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.
Bioorg Med Chem Lett 30: (2020)
University Of Bonn
Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
Eur J Med Chem 205: (2020)
Beni-Suef University
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (ROR?/RORc) inverse agonists.
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
Eur J Med Chem 205: (2020)
Daegu-Gyeongbuk Medical Innovation Foundation
Research advances on selective phosphatidylinositol 3 kinase ? (PI3K?) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Xi'An Jiaotong University
Identification of free fatty acid receptor 2 agonists using virtual screening.
Bioorg Med Chem Lett 30: 127460 (2020)
TBA
Structure activity study of S-trityl-cysteamine dimethylaminopyridine derivatives as SIRT2 inhibitors: Improvement of SIRT2 binding and inhibition.
Bioorg Med Chem Lett 30: (2020)
Science Farm
Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents.
Bioorg Med Chem Lett 30: (2020)
Atat£Rk University
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization.
Eur J Med Chem 205: (2020)
The First Affiliated Hospital Of Xi'An Jiaotong University
Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice.
Sci Transl Med 12: (2020)
Wichita State University
A cell-penetrant lactam-stapled peptide for targeting eIF4E protein-protein interactions.
Eur J Med Chem 205: (2020)
University Of Michigan
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.
Bioorg Med Chem Lett 30: (2020)
Dana-Farber Cancer Institute
Synthesis and biological evaluation of parthenolide derivatives with reduced toxicity as potential inhibitors of the NLRP3 inflammasome.
Bioorg Med Chem Lett 30: (2020)
Guangzhou Medical University
Structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling.
Bioorg Med Chem Lett 30: (2020)
Tokyo Medical And Dental University (Tmdu)
The transcriptional repressor REV-ERB as a novel target for disease.
Bioorg Med Chem Lett 30: (2020)
Imperial College London
5,5-Difluoro- and 5-Fluoro-5-methyl-hexose-based C-Glucosides as potent and orally bioavailable SGLT1 and SGLT2 dual inhibitors.
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp
Bioorg Med Chem Lett 30: (2020)
Takeda Research In California
Design, synthesis and biological evaluation of 2-indolinone derivatives as PAK1 inhibitors in MDA-MB-231 cells.
Bioorg Med Chem Lett 30: (2020)
Harbin Medical University
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Bioorg Med Chem Lett 30: (2020)
Merck
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Bioorg Med Chem Lett 30: (2020)
Genomics Institute Of The Novartis Research Foundation
Orally bioavailable HCV NS5A inhibitors of unsymmetrical structural class.
Bioorg Med Chem Lett 30: (2020)
Japan Tobacco
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Bioorg Med Chem Lett 30: (2020)
Merck
Topical 'dual-soft' glucocorticoid receptor agonist for dermatology.
Bioorg Med Chem Lett 30: (2020)
Leo Pharma
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel ROR?t inverse agonists.
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.
Bioorg Med Chem Lett 30: (2020)
Zhejiang Ocean University
Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
Eur J Med Chem 204: (2020)
Shenyang Pharmaceutical University
Synthesis, inhibitory activity and in silico docking of dual COX/5-LOX inhibitors with quinone and resorcinol core.
Eur J Med Chem 204: (2020)
Institute Of Experimental Botany Of The Czech Academy Of Sciences
Design, synthesis and in vitro cell-free/cell-based biological evaluations of novel ERCC1-XPF inhibitors targeting DNA repair pathway.
Eur J Med Chem 204: (2020)
University Of Alberta
Synthesis and biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors.
Eur J Med Chem 205: (2020)
Shanghai Jiao Tong University
Bioisosteric substitution of adamantane with bicyclic lipophilic groups improves water solubility of human soluble epoxide hydrolase inhibitors.
Bioorg Med Chem Lett 30: (2020)
University Of California Davis
New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.
Bioorg Med Chem Lett 30: (2020)
Gedeon Richter
Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable ROR?t inverse agonists.
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Development of SKI-349, a dual-targeted inhibitor of sphingosine kinase and microtubule polymerization.
Bioorg Med Chem Lett 30: (2020)
Pennsylvania State University College Of Medicine
Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome.
Eur J Med Chem 204: (2020)
Palack£
Design, synthesis and biological activities of novel pleuromutilin derivatives with a substituted triazole moiety as potent antibacterial agents.
Eur J Med Chem 204: (2020)
South China Agricultural University
Identification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo.
Eur J Med Chem 204: (2020)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer.
Eur J Med Chem 204: (2020)
Zhuhai Campus Of Zunyi Medical University
New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines.
Bioorg Med Chem Lett 30: (2020)
Gedeon Richter
Exploiting binding-site arginines in drug design: Recent examples.
Bioorg Med Chem Lett 30: (2020)
Prelude Therapeutics
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Design and synthesis of peptidic partial agonists of human neuromedin U receptor 1 with enhanced serum stability.
Bioorg Med Chem Lett 30: (2020)
Tokyo University Of Pharmacy And Life Sciences
Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines.
Bioorg Med Chem Lett 30: (2020)
University Of Rijeka
The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38? MAP kinase inhibitors.
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Development of chiral fluorinated alkyl derivatives of emixustat as drug candidates for the treatment of retinal degenerative diseases.
Bioorg Med Chem Lett 30: (2020)
Bar-Ilan University
Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer's disease.
Bioorg Med Chem Lett 30: (2020)
Viet Nam
Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.
Eur J Med Chem 203: (2020)
University Of Arkansas For Medical Sciences
Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators.
Eur J Med Chem 204: (2020)
Xiamen University
Benzothiophene-2-carboxamide derivatives as SENPs inhibitors with selectivity within SENPs family.
Eur J Med Chem 204: (2020)
Shanghai Jiao Tong University
Designing an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells.
Eur J Med Chem 204: (2020)
Sichuan University
Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
Eur J Med Chem 204: (2020)
Universidade Federal Do Rio De Janeiro
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.
Eur J Med Chem 204: (2020)
Guizhou Medical University
Synthesis and matched molecular pair analysis of covalent reversible inhibitors of the cysteine protease CPB.
Bioorg Med Chem Lett 30: (2020)
S£O Carlos Institute Of Chemistry-University Of S£O Paulo (Iqsc-Usp)
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
Eur J Med Chem 202: (2020)
Sichuan University
Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer.
Eur J Med Chem 202: (2020)
Alma Mater Studiorum-Universit£
Automated design and optimization of multitarget schizophrenia drug candidates by deep learning.
Eur J Med Chem 204: (2020)
Shanghai Institute Of Materia Medica
Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents.
Eur J Med Chem 202: (2020)
Universit£
Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes.
Eur J Med Chem 203: (2020)
East China University Of Science And Technology
Stepwise Design of ?-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.
J Med Chem 63: 8534-8553 (2020)
F. Hoffmann-La Roche
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.
J Med Chem 63: 9360-9390 (2020)
University Of Barcelona (Ub)
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.
Eur J Med Chem 203: (2020)
Jinan University
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
J Med Chem 63: 9093-9126 (2020)
Glaxosmithkline
Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability.
Eur J Med Chem 203: (2020)
Taisho Pharmaceutical
Discovery of carboxyl-containing biaryl ureas as potent ROR?t inverse agonists.
Eur J Med Chem 202: (2020)
Fudan University
Design, Synthesis, and Evaluation of New Quinazolinone Derivatives that Inhibit Bloom Syndrome Protein (BLM) Helicase, Trigger DNA Damage at the Telomere Region, and Synergize with PARP Inhibitors.
J Med Chem 63: 9752-9772 (2020)
Sun Yat-Sen University
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
J Med Chem 63: 12526-12541 (2020)
Biogen
Discovery and Characterization of Pure RhlR Antagonists against
J Med Chem 63: 8388-8407 (2020)
Korea University
Chlorine substituents and linker topology as factors of 5-HT
Eur J Med Chem 203: (2020)
Jagiellonian University
Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
J Med Chem 63: 13258-13265 (2020)
Centre D'Etude Des Pathologies Respiratoires And Universit£
Recent Progress in the Discovery of Antifungal Agents Targeting the Cell Wall.
J Med Chem 63: 12429-12459 (2020)
Shaanxi University Of Science And Technology
Design and Synthesis of a Highly Selective and
J Med Chem 63: 9070-9092 (2020)
Glaxosmithkline
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
J Med Chem 63: 9045-9069 (2020)
Glaxosmithkline
Design, synthesis and biological evaluation of novel glyoxalase I inhibitors possessing diazenylbenzenesulfonamide moiety as potential anticancer agents.
Bioorg Med Chem 28: (2020)
Jordan University Of Science And Technology
Synthesis of 2-guanidinyl pyridines and their trypsin inhibition and docking.
Bioorg Med Chem 28: (2020)
University College Dublin
Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL).
Bioorg Med Chem 28: (2020)
Graz University Of Technology
Modulation of TRPV4 and BKCa for treatment of brain diseases.
Bioorg Med Chem 28: (2020)
Kunming University Of Science And Technology
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.
Bioorg Med Chem 28: (2020)
Chinese Academy Of Medical Science And Peking Union Medical College
An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators.
Bioorg Med Chem 28: (2020)
Shandong University
Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors.
Bioorg Med Chem 28: (2020)
University Of Iowa
Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.
Bioorg Med Chem 28: (2020)
Southern Medical University
Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.
J Med Chem 63: 9512-9522 (2020)
Virginia Commonwealth University
Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile.
Eur J Med Chem 203: (2020)
University Of Defense
Development of dual inhibitors targeting pyruvate dehydrogenase kinases and human lactate dehydrogenase A: High-throughput virtual screening, synthesis and biological validation.
Eur J Med Chem 203: (2020)
Chongqing University
Design and Structural Optimization of Dual FXR/PPAR? Activators.
J Med Chem 63: 8369-8379 (2020)
Goethe University Frankfurt
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
J Med Chem 63: 12290-12358 (2020)
University Of Nebraska Medical Center
Photoswitchable Antagonists for a Precise Spatiotemporal Control of ?
J Med Chem 63: 8458-8470 (2020)
Institute For Advanced Chemistry Of Catalonia (Iqac-Csic)
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells.
Eur J Med Chem 203: (2020)
Taipei Medical University
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Eur J Med Chem 203: (2020)
Chinese Academy Of Sciences
Development of a metabolically stable topoisomerase I poison as anticancer agent.
Eur J Med Chem 202: (2020)
Csir-Indian Institute Of Chemical Biology
Amphiphilic aminoglycosides with increased selectivity for inhibition of connexin 43 (Cx43) hemichannels.
Eur J Med Chem 203: (2020)
Utah State University
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.
Eur J Med Chem 203: (2020)
Jiangxi Science & Technology Normal University
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.
Eur J Med Chem 203: (2020)
Hangzhou Institute Of Innovative Medicine
Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials.
J Med Chem 63: 11585-11601 (2020)
The University Of Sydney
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
ACS Med Chem Lett 11: 1484-1489 (2020)
University Of Texas Md Anderson Cancer Center
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
ACS Med Chem Lett 11: 1476-1483 (2020)
Merck
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.
ACS Med Chem Lett 11: 1470-1475 (2020)
University "G. D'Annunzio" Of Chieti-Pescara
Discovery of 3-Quinazolin-4(3
ACS Med Chem Lett 11: 1463-1469 (2020)
Luoxin Pharmaceutical (Shanghai) Co.
Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor.
ACS Med Chem Lett 11: 1429-1434 (2020)
National Center For Scientific Research Demokritos
Designing Dihydrofolate Reductase Inhibitors as X-ray Radiosensitizers to Reverse Radioresistance of Cervical Cancer.
ACS Med Chem Lett 11: 1421-1428 (2020)
Jinan University
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.
ACS Med Chem Lett 11: 1402-1409 (2020)
Biocon Bristol Myers Squibb Research Center
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase ?.
ACS Med Chem Lett 11: 1386-1391 (2020)
Gsk Medicines Research Centre
Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT
Eur J Med Chem 201: (2020)
Jagiellonian University Medical College
Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods.
J Med Chem 63: 8325-8337 (2020)
Vanderbilt University School Of Medicine
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.
J Med Chem 63: 12387-12402 (2020)
Research Triangle Institute
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
J Med Chem 63: 8296-8313 (2020)
University Of Massachusetts Medical School
Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.
J Med Chem 63: 8634-8648 (2020)
University Of Toronto Mississauga
Modulating microRNA Processing: Enoxacin, the Progenitor of a New Class of Drugs.
J Med Chem 63: 12275-12289 (2020)
University Of Perugia
Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors.
Eur J Med Chem 202: (2020)
Univ Angers
Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents.
J Med Chem 63: 8338-8358 (2020)
Southern Medical University
Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.
J Med Chem 63: 8584-8607 (2020)
Rapt Therapeutics
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
J Med Chem 63: 10773-10781 (2020)
Genomics Institute Of The Novartis Research Foundation (Gnf)
Discovery of an Orally Active Small-Molecule Tumor Necrosis Factor-? Inhibitor.
J Med Chem 63: 8146-8156 (2020)
Huazhong University Of Science And Technology
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
J Med Chem 63: 9316-9339 (2020)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent
J Med Chem 63: 9523-9539 (2020)
University Of Dundee
Discovery of first-in-class multi-target adenosine A
Eur J Med Chem 201: (2020)
Universit£
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.
Eur J Med Chem 201: (2020)
Universit£
The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.
J Med Chem 63: 8314-8324 (2020)
University Of Tennessee
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.
J Med Chem 63: 8567-8583 (2020)
Tsinghua University
Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2.
Eur J Med Chem 202: (2020)
Cnrs
Kojic acid-natural product conjugates as mushroom tyrosinase inhibitors.
Eur J Med Chem 201: (2020)
Mazandaran University Of Medical Sciences
Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-? aggregation against Alzheimer's disease.
Eur J Med Chem 202: (2020)
Affiated Tumor Hospital Of Guangxi Medical University
Synthesis of the Major Mammalian Metabolites of THCV.
J Nat Prod 83: 2060-2065 (2020)
National Research Council Of Italy
Tideglusib and Its Analogues As Inhibitors of
J Med Chem 63: 8442-8457 (2020)
Guizhou University
Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential.
Eur J Med Chem 202: (2020)
Bharati Vidyapeeth'S College Of Pharmacy
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
J Med Chem 63: 7773-7816 (2020)
Novartis Institutes For Biomedical Research
Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols.
Bioorg Med Chem 28: (2020)
251 General Air Force Hospital
Design, synthesis and biological activity of novel substituted 3-benzoic acid derivatives as MtDHFR inhibitors.
Bioorg Med Chem 28: (2020)
University Hospital T£Bingen
Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies.
Bioorg Med Chem 28: (2020)
Central University Of Punjab
Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-?-lactamases.
Bioorg Med Chem 28: (2020)
Uit The Arctic University Of Norway
Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.
Bioorg Med Chem 28: (2020)
Federal University Of S£O Carlos
Amide derivatives of Gallic acid: Design, synthesis and evaluation of inhibitory activities against in vitro ?-synuclein aggregation.
Bioorg Med Chem 28: (2020)
Zhengzhou University
New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation.
Bioorg Med Chem 28: (2020)
National Institute Of Pharmaceutical Education And Research (Niper)
Phenyltriazole-functionalized sulfamate inhibitors targeting tyrosyl- or isoleucyl-tRNA synthetase.
Bioorg Med Chem 28: (2020)
Ku Leuven
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT
Bioorg Med Chem 28: (2020)
City University Of New York
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTR
Bioorg Med Chem Lett 30: (2020)
Dominican College
Improving NK1R-targeted gene delivery of stearyl-antimicrobial peptide CAMEL by conjugating it with substance P.
Bioorg Med Chem Lett 30: (2020)
Lanzhou University
A chalcone derivative binds a putative allosteric site of YopH: Inhibition of a virulence factor of Yersinia.
Bioorg Med Chem Lett 30: (2020)
Universidade Federal De Santa Catarina
SAR of non-hydrolysable analogs of pyridoxal 5'-phosphate against low molecular weight protein tyrosine phosphatase isoforms.
Bioorg Med Chem Lett 30: (2020)
Saint John'S University
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-? (TGF-?) type I receptor inhibitors.
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Cairo University
Design, synthesis and biological evaluation of novel pteridinone derivatives possessing a hydrazone moiety as potent PLK1 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of 2-methyl-(1,1'-biphenyl)-pyrimidine conjugates.
Bioorg Med Chem Lett 30: (2020)
Zhejiang University
Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation.
Bioorg Med Chem Lett 30: (2020)
East China University Of Science & Technology
Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines.
Bioorg Med Chem Lett 30: (2020)
City University Of New York
Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ?FosB homodimers and ?FosB/JunD heterodimers.
Bioorg Med Chem Lett 30: (2020)
University Of Texas Medical Branch
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
Bioorg Med Chem Lett 30: (2020)
M. V. Lomonosov Moscow State University
Development of a new class of liver receptor homolog-1 (LRH-1) agonists by photoredox conjugate addition.
Bioorg Med Chem Lett 30: (2020)
Emory University
Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.
Bioorg Med Chem Lett 30: (2020)
Sabila Biosciences
C2-substituted quinazolinone derivatives exhibit A
Bioorg Med Chem Lett 30: (2020)
North-West University
Discovery of 5-(4-methylpiperazin-1-yl)-2-nitroaniline derivatives as a new class of SIRT6 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Sichuan University
A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis.
Eur J Med Chem 202: (2020)
Ochsner Clinic
Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H
Eur J Med Chem 202: (2020)
Xuzhou Medical University
Design, synthesis and evaluation of carbamate-linked uridyl-based inhibitors of human ST6Gal I.
Bioorg Med Chem 28: (2020)
University Of Wollongong
Bisphosphonate esters interact with HMG-CoA reductase membrane domain to induce its degradation.
Bioorg Med Chem 28: (2020)
The University Of Tokyo
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.
Bioorg Med Chem 28: (2020)
University Of Florida
2?-3,4-Unsaturated sialic acid derivatives: Synthesis optimization, and biological evaluation as Newcastle disease virus hemagglutinin-neuraminidase inhibitors.
Bioorg Med Chem 28: (2020)
University Of Milan
PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.
Eur J Med Chem 201: (2020)
University Of Toronto Mississauga
Discovery of AB680: A Potent and Selective Inhibitor of CD73.
J Med Chem 63: 11448-11468 (2020)
Arcus Biosciences
Oligopeptides as Neuropeptide Y Y
J Med Chem 63: 8198-8215 (2020)
University Of Regensburg
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
J Med Chem 63: 12460-12484 (2020)
University Of East Anglia
Amino Acids Bearing Aromatic or Heteroaromatic Substituents as a New Class of Ligands for the Lysosomal Sialic Acid Transporter Sialin.
J Med Chem 63: 8231-8249 (2020)
Universit£
A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays.
J Med Chem 63: 8179-8197 (2020)
Heidelberg University
Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues.
J Med Chem 63: 8419-8431 (2020)
Purdue University
Rational modification, synthesis and biological evaluation of 3,4-dihydroquinoxalin-2(1H)-one derivatives as potent and selective c-Jun N-terminal kinase 3 (JNK3) inhibitors.
Eur J Med Chem 201: (2020)
Peking University
Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.
Eur J Med Chem 201: (2020)
Shanghai University Of Traditional Chinese Medicine
Discovery of Novel PDE? Degraders for the Treatment of KRAS Mutant Colorectal Cancer.
J Med Chem 63: 7892-7905 (2020)
Second Military Medical University
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.
J Med Chem 63: 7867-7879 (2020)
Sun Yat-Sen University
A Venomics Approach Coupled to High-Throughput Toxin Production Strategies Identifies the First Venom-Derived Melanocortin Receptor Agonists.
J Med Chem 63: 8250-8264 (2020)
Universit£
Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors.
Eur J Med Chem 201: (2020)
Spanish National Cancer Research Centre (Cnio)
Rosuvastatin based novel 3-substituted isocoumarins / 3-alkylidenephthalides: Ultrasound assisted synthesis and identification of new anticancer agents.
Eur J Med Chem 201: (2020)
University Of Hyderabad Campus
Hydroxy-
J Nat Prod 83: 2212-2220 (2020)
Universidad Nacional Aut£Noma De M£Xico
Development of Conformationally Constrained ?-RgIA Analogues as Stable Peptide Antagonists of Human ?9?10 Nicotinic Acetylcholine Receptors.
J Med Chem 63: 8380-8387 (2020)
University Of Utah
Structural and Mechanistic Basis of the Inhibitory Potency of Selected 2-Aminothiazole Compounds on Protein Kinase CK2.
J Med Chem 63: 7766-7772 (2020)
Universit£T Zu K£Ln
Characterization of Inhibition Reveals Distinctive Properties for Human and
J Med Chem 63: 7545-7558 (2020)
Georg-August-University G£Ttingen
Dehydrohispanolone Derivatives Attenuate the Inflammatory Response through the Modulation of Inflammasome Activation.
J Nat Prod 83: 2155-2164 (2020)
Universidad Complutense De Madrid (Ucm)
Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.
J Med Chem 63: 7840-7856 (2020)
X-Chem
EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.
J Med Chem 63: 7252-7267 (2020)
University Of Michigan
Novel Thienopyrimidine Inhibitors of
J Med Chem 63: 7740-7765 (2020)
Imperial College London
Development of small-molecule inhibitors of fatty acyl-AMP and fatty acyl-CoA ligases in Mycobacterium tuberculosis.
Eur J Med Chem 201: (2020)
University Of Minnesota
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A
J Med Chem 63: 7721-7739 (2020)
Uppsala University
Dual Targeting of Norepinephrine Transporter (NET) Function and Thyrointegrin ?v?3 Receptors in the Treatment of Neuroblastoma.
J Med Chem 63: 7653-7662 (2020)
Albany College Of Pharmacy And Health Sciences
Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
Eur J Med Chem 201: (2020)
China Medical University
The structure-based optimization of ?-sultone-fused pyrazoles as selective BuChE inhibitors.
Eur J Med Chem 201: (2020)
Anhui Medical University
Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT
J Med Chem 63: 7529-7544 (2020)
University Of Texas Medical Branch
Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
Eur J Med Chem 201: (2020)
University Of Montpellier
Structure-Based Drug Discovery of
J Med Chem 63: 7906-7920 (2020)
Sosei Heptares
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.
J Med Chem 63: 6959-6978 (2020)
Sun Yat-Sen University
Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy.
J Med Chem 63: 7143-7162 (2020)
Asahi Kasei Pharma
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
J Med Chem 63: 8088-8113 (2020)
Novartis Institutes For Biomedical Research
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
ACS Med Chem Lett 11: 1342-1347 (2020)
Genentech
ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
ACS Med Chem Lett 11: 1335-1341 (2020)
Ono Pharmaceutical
Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel ?-Arrestin Antagonist Activity.
ACS Med Chem Lett 11: 1330-1334 (2020)
Pfizer
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.
ACS Med Chem Lett 11: 1324-1329 (2020)
Constellation Pharmaceuticals
Discovery of Novel Nonpeptidic PAR2 Ligands.
ACS Med Chem Lett 11: 1316-1323 (2020)
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)
Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1.
ACS Med Chem Lett 11: 1305-1309 (2020)
H3 Biomedicine
P2Y
ACS Med Chem Lett 11: 1281-1286 (2020)
Saint Louis University School Of Medicine
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.
ACS Med Chem Lett 11: 1269-1273 (2020)
Dana-Farber Cancer Institute
Discovery of RO7185876, a Highly Potent ?-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
ACS Med Chem Lett 11: 1257-1268 (2020)
F. Hoffmann-La Roche
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from
ACS Med Chem Lett 11: 1250-1256 (2020)
Brazilian Biosciences National Laboratory
Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase.
ACS Med Chem Lett 11: 1244-1249 (2020)
Goethe-University
Discovery of an Atropisomeric PI3K? Selective Inhibitor through Optimization of the Hinge Binding Motif.
ACS Med Chem Lett 11: 1236-1243 (2020)
Gilead Sciences
Benzoxazepine-Derived Selective, Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase.
ACS Med Chem Lett 11: 1228-1235 (2020)
Oncoarendi Therapeutics
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.
ACS Med Chem Lett 11: 1221-1227 (2020)
Bristol Myers Squibb
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
ACS Med Chem Lett 11: 1213-1220 (2020)
Constellation Pharmaceuticals
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
ACS Med Chem Lett 11: 1205-1212 (2020)
Constellation Pharmaceuticals
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.
ACS Med Chem Lett 11: 1196-1204 (2020)
Chinese Academy Of Medical Science And Peking Union Medical College
Scaffold Repurposing of in-House Chemical Library toward the Identification of New Casein Kinase 1 ? Inhibitors.
ACS Med Chem Lett 11: 1168-1174 (2020)
University Of Padova
Discovery of a Potent Dual Inhibitor of Wild-Type and Mutant Respiratory Syncytial Virus Fusion Proteins.
ACS Med Chem Lett 11: 1145-1151 (2020)
Taisho Pharmaceutical
Identification of Inhibitors of Thrombospondin 1 Activation of TGF-?.
ACS Med Chem Lett 11: 1130-1136 (2020)
Southern Research Institute
Design and Synthesis of Tetrazole- and Pyridine-Containing Itraconazole Analogs as Potent Angiogenesis Inhibitors.
ACS Med Chem Lett 11: 1111-1117 (2020)
Johns Hopkins School Of Medicine
Ligand Design for Cereblon Based Immunomodulatory Therapy.
ACS Med Chem Lett 11: 1088-1089 (2020)
Usona Institute
Cancer Immunotherapy through the Inhibition of Diacylglycerol Kinases Alpha and Zeta.
ACS Med Chem Lett 11: 1083-1085 (2020)
Therachem Research Medilab
Potential Cancer Treatment by Agonists of the Stimulator of Interferon Genes.
ACS Med Chem Lett 11: 1081-1082 (2020)
Therachem Research Medilab
Inhibitors of Hypoxia-Inducible Factors as Treatment for Cancer.
ACS Med Chem Lett 11: 1079-1080 (2020)
Therachem Research Medilab
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
A critical update on the strategies towards modulators targeting androgen receptors.
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein-Protein Inhibitors: Two Test Cases Illustrated by IL1?-IL1R and p38?-TAB1 Complexes.
J Med Chem 63: 7559-7568 (2020)
King'S College London
Fragment Linking Strategies for Structure-Based Drug Design.
J Med Chem 63: 11420-11435 (2020)
Universit£
Targeting Peroxisome Proliferator-Activated Receptor Delta (PPAR?): A Medicinal Chemistry Perspective.
J Med Chem 63: 10109-10134 (2020)
Daegu-Gyeongbuk Medical Innovation Foundation
Discovery of Dihydropyrrolo[1,2-
J Med Chem 63: 7569-7600 (2020)
Emory University
Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
Eur J Med Chem 201: (2020)
Shenyang Pharmaceutical University
Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
J Med Chem 63: 6876-6897 (2020)
TBA
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6
J Med Chem 63: 7817-7826 (2020)
Harvard Medical School
Synthesis and Structure-Activity Relationships of 5'-Aryl-14-alkoxypyridomorphinans: Identification of a ? Opioid Receptor Agonist/? Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects.
J Med Chem 63: 7663-7694 (2020)
University Of Alabama At Birmingham
Rapid Elaboration of Fragments into Leads by X-ray Crystallographic Screening of Parallel Chemical Libraries (REFiL
J Med Chem 63: 6863-6875 (2020)
Monash University (Parkville Campus)
Discovery of quinoline-based irreversible BTK inhibitors.
Bioorg Med Chem Lett 30: (2020)
Acerta Pharma
A cell-based fluorescent assay for FAP inhibitor discovery.
Bioorg Med Chem Lett 30: (2020)
Peking University First Hospital
Design, synthesis and evaluation of pyrazolopyrimidinone derivatives as novel PDE9A inhibitors for treatment of Alzheimer's disease.
Bioorg Med Chem Lett 30: (2020)
Sun Yat-Sen University
Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition.
Bioorg Med Chem Lett 30: (2020)
Prof John Barnabas Post Graduate School Of Biological Studies
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Bioorg Med Chem Lett 30: (2020)
Amgen
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Azetidine-based selective glycine transporter-1 (GlyT1) inhibitors with memory enhancing properties.
Bioorg Med Chem Lett 30: (2020)
Dart Neuroscience
Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents.
Bioorg Med Chem Lett 30: (2020)
Bengbu Medical College
Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting.
Bioorg Med Chem Lett 30: (2020)
Mansoura University
Discovery of hydroxy pyrimidine Factor IXa inhibitors.
Bioorg Med Chem Lett 30: (2020)
Merck
Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators.
Bioorg Med Chem Lett 30: (2020)
Chiba University
Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
Eur J Med Chem 201: (2020)
University Of Perugia
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding.
J Med Chem 63: 8857-8866 (2020)
Google Research Applied Science, Mountain View, California 94043, United States.
Antiproliferative Flavanoid Dimers Isolated from Brazilian Red Propolis.
J Nat Prod 83: 1784-1793 (2020)
Universidade De S£O Paulo
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.
J Med Chem 63: 6924-6940 (2020)
Ocean University Of China
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.
J Med Chem 63: 7422-7444 (2020)
University Of Firenze
New Broad-Spectrum Antibiotics Containing a Pyrrolobenzodiazepine Ring with Activity against Multidrug-Resistant Gram-Negative Bacteria.
J Med Chem 63: 6941-6958 (2020)
King'S College London
Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-
J Med Chem 63: 7369-7391 (2020)
University Of Siena
On the Promise of Photopharmacology Using Photoswitches: A Medicinal Chemist's Perspective.
J Med Chem 63: 11436-11447 (2020)
Imperial College London
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
J Med Chem 63: 11397-11419 (2020)
Norman Drug Discovery Training And Consulting
Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
J Med Chem 63: 6834-6846 (2020)
University Of Oslo
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
J Med Chem 63: 7163-7185 (2020)
Japan Tobacco
Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases.
J Med Chem 63: 7033-7051 (2020)
The First Affiliated Hospital Of Xi'An Jiao Tong University
Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold.
Eur J Med Chem 200: (2020)
University Of Houston
Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction.
Eur J Med Chem 200: (2020)
Harbin Institute Of Technology
Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors.
Bioorg Med Chem 28: (2020)
Tufts University
Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
Bioorg Med Chem 28: (2020)
Zhejiang University
Synthesis of novel 3,5,6-trisubstituted 2-pyridone derivatives and evaluation for their anti-inflammatory activity.
Bioorg Med Chem 28: (2020)
Universidade Estadual De Maring£
The synthesis and biological evaluation of nucleobases/tetrazole hybrid compounds: A new class of phosphodiesterase type 3 (PDE3) inhibitors.
Bioorg Med Chem 28: (2020)
Shiraz University
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).
Bioorg Med Chem 28: (2020)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.
Bioorg Med Chem 28: (2020)
Duquesne University
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
J Med Chem 63: 6708-6726 (2020)
Harvard Medical School
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
J Med Chem 63: 7293-7325 (2020)
Bayer
N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies.
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
Eur J Med Chem 200: (2020)
Martin-Luther University Of Halle-Wittenberg
Structural Revision of Garcinielliptin Oxide and Garcinielliptone E.
J Nat Prod 83: 2041-2044 (2020)
University Of Kentucky
Inhibiting Matrix Metalloproteinase-2 Activation by Perturbing Protein-Protein Interactions Using a Cyclic Peptide.
J Med Chem 63: 6979-6990 (2020)
University Of California
Discovery and Structural Optimization of 4-(Aminomethyl)benzamides as Potent Entry Inhibitors of Ebola and Marburg Virus Infections.
J Med Chem 63: 7211-7225 (2020)
University Of Illinois At Chicago
Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity.
Eur J Med Chem 200: (2020)
National Center For Radiation Research And Technology (Ncrrt)
Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
Eur J Med Chem 200: (2020)
Alexandria University
Design and Synthesis of a Trifunctional Molecular System "Programmed" to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells.
J Med Chem 63: 5752-5762 (2020)
The Research Institute Of The Mcgill University Health Center/Glen Hospital
Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.
J Med Chem 63: 10533-10593 (2020)
Taipei Medical University
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
Eur J Med Chem 200: (2020)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great
J Med Chem 63: 7326-7346 (2020)
Shenyang Pharmaceutical University
Identification of
J Med Chem 63: 6748-6773 (2020)
China Pharmaceutical University
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
J Med Chem 63: 5879-5955 (2020)
Inception Therapeutics
-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting
J Med Chem 63: 8359-8368 (2020)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips) - Helmholtz Centre For Infection Research (Hzi
Precursor-Directed Biosynthesis and Fluorescence Labeling of Clickable Microcystins.
J Nat Prod 83: 1960-1970 (2020)
University Of Halle-Wittenberg
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
J Med Chem 63: 12213-12242 (2020)
University Of Leeds
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.
J Med Chem 63: 11305-11329 (2020)
China Pharmaceutical University
Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors.
J Med Chem 63: 7392-7409 (2020)
Universit£
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.
J Med Chem 63: 7008-7032 (2020)
Gvk Biosciences
Bioisosteric Replacement of Arylamide-Linked Spine Residues with
J Med Chem 63: 7347-7354 (2020)
Federal University Of Rio De Janeiro (Ufrj)
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H
J Med Chem 63: 7268-7292 (2020)
Pfizer
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application.
J Med Chem 63: 11368-11396 (2020)
China Pharmaceutical University
Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII.
Eur J Med Chem 200: (2020)
Latvian Institute Of Organic Synthesis
Matrix Metalloproteinases as New Targets in Alzheimer's Disease: Opportunities and Challenges.
J Med Chem 63: 10705-10725 (2020)
Normandie Univ
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
J Med Chem 63: 7226-7242 (2020)
Bristol Myers Squibb
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.
Eur J Med Chem 200: (2020)
Northwest A&F University
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
J Med Chem 63: 7186-7210 (2020)
University Of Illinois At Chicago
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
J Med Chem 63: 7108-7126 (2020)
Haisco Pharmaceutical Group
Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups.
Eur J Med Chem 200: (2020)
Consejo Superior De Investigaciones Cient�Ficas (Iqm-Csic)
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.
Eur J Med Chem 200: (2020)
China Pharmaceutical University
DDX3X inhibitors, an effective way to overcome HIV-1 resistance targeting host proteins.
Eur J Med Chem 200: (2020)
Universit£
Privileged scaffold-based design to identify a novel drug-like 5-HT
Eur J Med Chem 199: (2020)
Universit£
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein.
J Med Chem 63: 7510-7528 (2020)
TBA
Factor H-Inspired Design of Peptide Biomarkers of the Complement C3d Protein.
ACS Med Chem Lett 11: 1054-1059 (2020)
University Of California Riverside
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
ACS Med Chem Lett 11: 1047-1053 (2020)
University Of Naples "Federico Ii
Discovery of Small-Molecule Stabilizers of 14-3-3 Protein-Protein Interactions via Dynamic Combinatorial Chemistry.
ACS Med Chem Lett 11: 1041-1046 (2020)
University Of Groningen
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents.
ACS Med Chem Lett 11: 1028-1034 (2020)
University Of Modena And Reggio Emilia
Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer.
ACS Med Chem Lett 11: 1022-1027 (2020)
Kafrelsheikh University
Phenolic Compounds from
ACS Med Chem Lett 11: 1006-1013 (2020)
Centre Of Experimental Medicine
Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms.
ACS Med Chem Lett 11: 1000-1005 (2020)
Universit£
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
ACS Med Chem Lett 11: 977-983 (2020)
Sapienza University Of Rome
Structure-Guided Identification of DNMT3B Inhibitors.
ACS Med Chem Lett 11: 971-976 (2020)
Yale University
Progress in the Field of Aldehyde Dehydrogenase Inhibitors: Novel Imidazo[1,2-
ACS Med Chem Lett 11: 963-970 (2020)
University Of Pisa
Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor.
ACS Med Chem Lett 11: 956-962 (2020)
Universit£
Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation.
ACS Med Chem Lett 11: 889-894 (2020)
University Of Catania
Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.
ACS Med Chem Lett 11: 869-876 (2020)
University Of Bari Aldo Moro
From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.
ACS Med Chem Lett 11: 862-868 (2020)
University Of Naples
New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII.
ACS Med Chem Lett 11: 852-856 (2020)
University Of Cagliari
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and
ACS Med Chem Lett 11: 825-831 (2020)
Angelini Pharma
GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis.
ACS Med Chem Lett 11: 818-824 (2020)
University Of Naples "Federico Ii
Peptides Mimicking the ?7/?8 Loop of HIV-1 Reverse Transcriptase p51 as "Hotspot-Targeted" Dimerization Inhibitors.
ACS Med Chem Lett 11: 811-817 (2020)
Instituto De Qu£Mica M£Dica (Iqm, Csic)
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of
ACS Med Chem Lett 11: 806-810 (2020)
University Of Messina
Pyrrolyl Pyrazoles as Non-Diketo Acid Inhibitors of the HIV-1 Ribonuclease H Function of Reverse Transcriptase.
ACS Med Chem Lett 11: 798-805 (2020)
"Sapienza" Universit£
Targeting mPGES-1 by a Combinatorial Approach: Identification of the Aminobenzothiazole Scaffold to Suppress PGE
ACS Med Chem Lett 11: 783-789 (2020)
University Of Salerno
5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.
ACS Med Chem Lett 11: 766-772 (2020)
Irbm
Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.
ACS Med Chem Lett 11: 754-759 (2020)
European Institute Of Oncology Irccs
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.
ACS Med Chem Lett 11: 740-746 (2020)
Irbm
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.
ACS Med Chem Lett 11: 732-739 (2020)
Alma Mater Studiorum-University Of Bologna
Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors.
ACS Med Chem Lett 11: 727-731 (2020)
Universit£
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.
ACS Med Chem Lett 11: 720-726 (2020)
Universit£
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
ACS Med Chem Lett 11: 713-719 (2020)
Universidad San Pablo-Ceu
Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor.
ACS Med Chem Lett 11: 706-712 (2020)
University Of Illinois At Chicago
Development of Pyrazolo[3,4-
ACS Med Chem Lett 11: 657-663 (2020)
University Of Genoa
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
ACS Med Chem Lett 11: 651-656 (2020)
University Of Trieste
Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors.
ACS Med Chem Lett 11: 633-637 (2020)
Sapienza University Of Rome
Sulfonimide and Amide Derivatives as Novel PPAR? Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.
ACS Med Chem Lett 11: 624-632 (2020)
"G. D'Annunzio" University Of Chieti-Pescara
Chimeric Peptidomimetics of SOCS 3 Able to Interact with JAK2 as Anti-inflammatory Compounds.
ACS Med Chem Lett 11: 615-623 (2020)
University Of Naples "Federico Ii
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity
J Med Chem 63: 6784-6801 (2020)
University Of Nottingham
High-Throughput Screening for the Discovery of Enzyme Inhibitors.
J Med Chem 63: 10742-10772 (2020)
University Of Bath
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
J Med Chem 63: 10726-10741 (2020)
Jinan University
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
J Med Chem 63: 5783-5796 (2020)
China Pharmaceutical University
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
Eur J Med Chem 199: (2020)
Central South University
Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease.
ACS Infect Dis 6: 2099-2109 (2020)
University Of Georgia
Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
Eur J Med Chem 198: (2020)
Newlink Genetics
Exploration of carbamide derived pyrimidine-thioindole conjugates as potential VEGFR-2 inhibitors with anti-angiogenesis effect.
Eur J Med Chem 200: (2020)
National Institute Of Pharmaceutical Education And Research (Niper)
Hybrid Screening Approach for Very Small Fragments: X-ray and Computational Screening on FKBP51.
J Med Chem 63: 5856-5864 (2020)
Boehringer Ingelheim Pharma
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H
J Med Chem 63: 5297-5311 (2020)
University Of Regensburg
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis.
J Med Chem 63: 6144-6163 (2020)
Washington University School Of Medicine
A ?-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli.
J Med Chem 63: 5990-6002 (2020)
Louis Stokes Cleveland Department Of Veterans Affairs Medical Center
Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
Eur J Med Chem 199: (2020)
Erciyes University
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
J Med Chem 63: 5816-5840 (2020)
Glaxosmithkline R&D
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1
J Med Chem 63: 8046-8058 (2020)
Janssen Pharmaceutical Companies Of Johnson & Johnson
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
J Med Chem 63: 10188-10203 (2020)
Gilead Sciences
Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
J Med Chem 63: 9003-9019 (2020)
Kyorin Pharmaceutical
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR
Eur J Med Chem 199: (2020)
Zhengzhou University
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.
Eur J Med Chem 199: (2020)
University Paris-Saclay
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Novel bacterial topoisomerase inhibitors derived from isomannide.
Eur J Med Chem 199: (2020)
The Ohio State University
Discovery of DS-1971a, a Potent, Selective Na
J Med Chem 63: 10204-10220 (2020)
Daiichi Sankyo
-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity.
J Med Chem 63: 5734-5751 (2020)
Universidad De Granada
Structure-Activity Relationship Study Enables the Discovery of a Novel
J Med Chem 63: 5841-5855 (2020)
Xiamen University
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures.
J Med Chem 63: 5865-5878 (2020)
Ocean University Of China
Non-'classical' MEKs: A review of MEK3-7 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Northwestern University
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.
Bioorg Med Chem 28: (2020)
Bristol Myers Squibb
Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1.
Eur J Med Chem 199: (2020)
Southern Medical University
Discovery of bazedoxifene analogues targeting glycoprotein 130.
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Rational design and biological evaluation of gemfibrozil modified Xenopus GLP-1 derivatives as long-acting hypoglycemic agents.
Eur J Med Chem 198: (2020)
Jiangnan University
Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease.
Eur J Med Chem 198: (2020)
Universidad De Chile
Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate.
Eur J Med Chem 198: (2020)
Anadolu University
Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-? type 1 receptor inhibitors.
Eur J Med Chem 198: (2020)
China Pharmaceutical University
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective ? opioid receptor antagonists.
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.
J Med Chem 63: 5956-5971 (2020)
The University Of Queensland
Synthesis, biochemical evaluation, and molecular modeling of organophosphate-coumarin hybrids as potent and selective butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 30: (2020)
California State University
New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation.
Eur J Med Chem 198: (2020)
Sapienza University Of Rome
N-alkylpiperidine carbamates as potential anti-Alzheimer's agents.
Eur J Med Chem 197: (2020)
University Of Ljubljana
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF
J Med Chem 63: 6225-6237 (2020)
Westf£Lische Wilhelms-Universit£T M£Nster
Identification of the New Covalent Allosteric Binding Site of Fructose-1,6-bisphosphatase with Disulfiram Derivatives toward Glucose Reduction.
J Med Chem 63: 6238-6247 (2020)
Central China Normal University
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3K? inhibitors with potent antitumor activity.
Eur J Med Chem 197: (2020)
Guizhou Medical University
Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease.
Eur J Med Chem 198: (2020)
Indian Institute Of Technology (Banaras Hindu University)
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus.
J Med Chem 63: 5763-5782 (2020)
Universit£
Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights.
Bioorg Med Chem 28: (2020)
Jouf University
Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors.
Bioorg Med Chem Lett 30: (2020)
Sungkyunkwan University
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
J Med Chem 63: 4978-4996 (2020)
University Of Toronto
Discovery of Potent, Selective, and State-Dependent Na
J Med Chem 63: 6107-6133 (2020)
Lupin
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.
J Med Chem 63: 5477-5487 (2020)
Icahn School Of Medicine At Mount Sinai
Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.
Antimicrob Agents Chemother 64: (2020)
Institut Pasteur Korea
Learning Molecular Representations for Medicinal Chemistry.
J Med Chem 63: 8705-8722 (2020)
University Of California
Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.
J Med Chem 63: 5274-5286 (2020)
Monash University (Parkville Campus)
Structural Specificity of Flavonoids in the Inhibition of Human Fructose 1,6-Bisphosphatase.
J Nat Prod 83: 1541-1552 (2020)
University Of Porto
Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy.
J Med Chem 63: 5185-5200 (2020)
University Of Florence
Exploring tryptamine conjugates as pronucleotides of phosphate-modified 7-methylguanine nucleotides targeting cap-dependent translation.
Bioorg Med Chem 28: (2020)
University Of Warsaw
Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
Eur J Med Chem 198: (2020)
National Research Centre
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.
Eur J Med Chem 198: (2020)
Beijing University Of Chemical Technology
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?.
J Med Chem 63: 6727-6740 (2020)
Goethe-University Frankfurt
Design and synthesis of 1,3-benzothiazinone derivatives as potential anti-inflammatory agents.
Bioorg Med Chem 28: (2020)
Lanzhou University
Synthesis of morpholine derivatives using the Castagnoli-Cushman reaction as BACE1 inhibitors: Unexpected binding activity of cyclic thioamides.
Bioorg Med Chem Lett 30: (2020)
University Of Florence
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature 583: 459-468 (2020)
Qbi Covid-19 Research Group (Qcrg)
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
J Med Chem 63: 5421-5441 (2020)
East China Normal University
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
J Med Chem 63: 4867-4879 (2020)
Purdue University
Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.
J Nat Prod 83: 1461-1472 (2020)
Taipei Chang Gung Memorial Hospital
Discovery of Novel Fungal Lanosterol 14?-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
J Med Chem 63: 5341-5359 (2020)
Second Military Medical University
Discovery of novel, potent, and orally bioavailable pyrido[2,3-d][1]benzazepin-6-one antagonists for parathyroid hormone receptor 1.
Bioorg Med Chem 28: (2020)
Daiichi Sankyo
Secondary metabolites from Isodon ternifolius (D. Don) Kudo and their anticancer activity as DNA topoisomerase IB and Tyrosyl-DNA phosphodiesterase 1 inhibitors.
Bioorg Med Chem 28: (2020)
Sun Yat-Sen University
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
J Med Chem 63: 6164-6178 (2020)
University Of Bonn
Discovery of novel TNNI3K inhibitor suppresses pyroptosis and apoptosis in murine myocardial infarction injury.
Eur J Med Chem 197: (2020)
Sichuan University And Collaborative Innovation Center
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-?-d-Ribose Oxidase (DprE1) Inhibitors.
J Med Chem 63: 5367-5386 (2020)
University Of Antwerp
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
J Med Chem 63: 5526-5567 (2020)
National Institute Of Neurological Disorders And Stroke
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.
Bioorg Med Chem 28: (2020)
Universit£
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting
Bioorg Med Chem 28: (2020)
National Research Centre (Nrc Id: 60014618)
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Bioorg Med Chem Lett 30: (2020)
Merck
Synthesis and Biochemical Evaluation of Noncyclic Nucleotide Exchange Proteins Directly Activated by cAMP 1 (EPAC1) Regulators.
J Med Chem 63: 5159-5184 (2020)
University Of Texas Medical Branch
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong
J Med Chem 63: 4997-5010 (2020)
TBA
Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.
J Med Chem 63: 8025-8042 (2020)
Bayer
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.
J Med Chem 63: 5488-5500 (2020)
University Of Bath
Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential.
Bioorg Med Chem 28: (2020)
Universidade De Mogi Das Cruzes (Umc)
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t.
Bioorg Med Chem Lett 30: (2020)
Phenex Pharmaceuticals
The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL).
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach.
Bioorg Med Chem Lett 30: (2020)
Phenex Pharmaceuticals
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists.
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.
Eur J Med Chem 197: (2020)
University Of Colorado Anschutz Medical Campus
Monovalent protein-degraders - Insights and future perspectives.
Bioorg Med Chem Lett 30: (2020)
Cedilla Therapeutics
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Bioorg Med Chem Lett 30: (2020)
Merck
Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.
J Med Chem 63: 4957-4977 (2020)
Firmenich
Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design.
J Med Chem 63: 8956-8976 (2020)
TBA
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
J Med Chem 63: 5324-5340 (2020)
Yale University
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
J Med Chem 63: 5458-5476 (2020)
Chinese Academy Of Medical Sciences & Peking Union Medical College
An aza-nucleoside, fragment-like inhibitor of the DNA repair enzyme alkyladenine glycosylase (AAG).
Bioorg Med Chem 28: (2020)
University Of Surrey
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema.
Bioorg Med Chem 28: (2020)
University Of Michigan
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
Bioorg Med Chem 28: (2020)
Kyung Hee University
Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors.
Bioorg Med Chem 28: (2020)
Latvian Institute Of Organic Synthesis
Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors.
Eur J Med Chem 196: (2020)
Taipei Medical University
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.
J Med Chem 63: 10135-10157 (2020)
China Pharmaceutical University
Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease.
Science 368: 1331-1335 (2020)
Shanghai Institute Of Materia Medica
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
J Med Chem 63: 5501-5525 (2020)
Ocean University Of China
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
J Med Chem 63: 5212-5241 (2020)
University Of Strathclyde
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
J Med Chem 63: 8977-9002 (2020)
Shandong First Medical University & Shandong Academy Of Medical Sciences
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.
Bioorg Med Chem Lett 30: (2020)
Central South University
Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy.
J Med Chem 63: 5139-5158 (2020)
Dongguk University-Seoul
The Oxidation of Phytocannabinoids to Cannabinoquinoids.
J Nat Prod 83: 1711-1715 (2020)
Universit£
Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP.
J Med Chem 63: 4716-4731 (2020)
Avera Institute For Human Genetics
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
J Nat Prod 83: 1359-1367 (2020)
University Of Defence
Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for ?-secretase modulators with oral efficacy against cognitive deficits in Alzheimer's disease model mice.
Bioorg Med Chem 28: (2020)
Astellas Pharma
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity.
Bioorg Med Chem Lett 30: (2020)
Seoul National University
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity.
J Med Chem 63: 5398-5420 (2020)
Rapt Therapeutics
Triazolo-Peptidomimetics: Novel Radiolabeled Minigastrin Analogs for Improved Tumor Targeting.
J Med Chem 63: 4484-4495 (2020)
Eth Zurich
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
J Med Chem 63: 4824-4836 (2020)
University Of Washington
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.
J Med Chem 63: 4528-4554 (2020)
Northwestern University
A Chemical Switch for Transforming a Purine Agonist for Toll-like Receptor 7 to a Clinically Relevant Antagonist.
J Med Chem 63: 4776-4789 (2020)
Csir-Indian Institute Of Chemical Biology
Evaluation of nitrocatechol chalcone and pyrazoline derivatives as inhibitors of catechol-O-methyltransferase and monoamine oxidase.
Bioorg Med Chem Lett 30: (2020)
North-West University
Discovery of ? opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
Bioorg Med Chem Lett 30: (2020)
Kitasato University
Induction of enantio-selective apoptosis in human leukemia HL-60 cells by (S)-erypoegin K, an isoflavone isolated from Erythrina poeppigiana.
Bioorg Med Chem 28: (2020)
Meijo University
Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer's Disease.
J Med Chem 63: 6028-6056 (2020)
Czech Academy Of Sciences
Naphthacemycins from a
J Nat Prod 83: 1394-1399 (2020)
Hebei Medical University
Discovery and Structure-Activity Relationship Study of (
J Med Chem 63: 4880-4895 (2020)
Dana-Farber Cancer Institute
Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.
J Med Chem 63: 4506-4516 (2020)
Universit£
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
J Med Chem 63: 4790-4810 (2020)
Shandong University
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.
J Med Chem 63: 4849-4866 (2020)
Chinese Academy Of Sciences
Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist.
J Med Chem 63: 4762-4775 (2020)
University Of Texas Medical Branch
Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
Eur J Med Chem 195: (2020)
National Center For Genetic Engineering And Biotechnology (Biotec)
Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.
J Med Chem 63: 4837-4848 (2020)
Shandong University
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
ACS Med Chem Lett 11: 582-588 (2020)
Merck
Efficacy and Tolerability of Pyrazolo[1,5-
ACS Med Chem Lett 11: 558-565 (2020)
The Genomics Institute Of The Novartis Research Foundation
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
ACS Med Chem Lett 11: 550-557 (2020)
Merck
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
ACS Med Chem Lett 11: 541-549 (2020)
Genentech
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.
ACS Med Chem Lett 11: 535-540 (2020)
Jinan University
Discovery of [1,2,4]Triazolo[1,5-
ACS Med Chem Lett 11: 528-534 (2020)
Teijin Pharma
Synthesis and Evaluation of Noncovalent Naphthalene-Based KEAP1-NRF2 Inhibitors.
ACS Med Chem Lett 11: 521-527 (2020)
University Of Illinois At Chicago
Catching a Moving Target: Comparative Modeling of Flaviviral NS2B-NS3 Reveals Small Molecule Zika Protease Inhibitors.
ACS Med Chem Lett 11: 514-520 (2020)
Freie Universit£T Berlin
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
ACS Med Chem Lett 11: 506-513 (2020)
Gilead Sciences
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET
ACS Med Chem Lett 11: 497-505 (2020)
University Of Manchester
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.
ACS Med Chem Lett 11: 491-496 (2020)
University Of Oxford
Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors.
ACS Med Chem Lett 11: 485-490 (2020)
Biogen
Discovery and Pharmacokinetics of Sulfamides and Guanidines as Potent Human Arginase 1 Inhibitors.
ACS Med Chem Lett 11: 433-438 (2020)
Oncoarendi Therapeutics
Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis.
ACS Med Chem Lett 11: 419-425 (2020)
University Of Florida
Selective Estrogen Receptor Degraders for the Potential Treatment of Cancer.
ACS Med Chem Lett 11: 412-413 (2020)
Usona Institute
Bifunctional Pyrimidines as Modulators of Focal Adhesion Kinase.
ACS Med Chem Lett 11: 409-411 (2020)
Usona Institute
Cereblon Based Immunomodulatory Therapeutics.
ACS Med Chem Lett 11: 407-408 (2020)
Usona Institute
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.
J Med Chem 63: 4685-4700 (2020)
Central South University
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).
Eur J Med Chem 195: (2020)
Shanghai Institute Of Materia Medica
Both d- and l-Glucose Polyphosphates Mimic d-
J Med Chem 63: 5442-5457 (2020)
University Of Oxford
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
J Med Chem 63: 4171-4182 (2020)
Gwangju Institute Of Science And Technology
Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors.
Bioorg Med Chem 28: (2020)
North-West University
Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor ? (ER?) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer.
Eur J Med Chem 195: (2020)
Wuhan University
A novel class of selective CK2 inhibitors targeting its open hinge conformation.
Eur J Med Chem 195: (2020)
University Of Trento
Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus
J Nat Prod 83: 1258-1264 (2020)
Chinese Academy Of Sciences
Discovery and Optimization of Glucose Uptake Inhibitors.
J Med Chem 63: 5201-5211 (2020)
Kadmon
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
J Med Chem 63: 4579-4602 (2020)
Shanghaitech University
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.
Bioorg Med Chem 28: (2020)
Astellas Pharma
Screening of chalcone analogs with anti-depressant, anti-inflammatory, analgesic, and COX-2-inhibiting effects.
Bioorg Med Chem Lett 30: (2020)
China-Japan Union Hospital Of Jilin University
Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling.
Bioorg Med Chem Lett 30: (2020)
Wright State University
MymA Bioactivated Thioalkylbenzoxazole Prodrug Family Active against
J Med Chem 63: 4732-4748 (2020)
Glaxosmithkline
Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Jiangnan University
Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
Bioorg Med Chem Lett 30: (2020)
South China Sea Institute Of Oceanology
Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives.
Bioorg Med Chem Lett 30: (2020)
Khon Kaen University
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors
Nature 582: 289-293 (2020)
Shanghaitech University
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPAR? activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.
Eur J Med Chem 195: (2020)
University Of Innsbruck
Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia.
Eur J Med Chem 195: (2020)
Gwangju Institute Of Science And Technology
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
J Med Chem 63: 4334-4348 (2020)
Medical College Of Wisconsin
A Selective Modulator of Peroxisome Proliferator-Activated Receptor ? with an Unprecedented Binding Mode.
J Med Chem 63: 4555-4561 (2020)
Goethe-University Frankfurt
Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma.
J Med Chem 63: 4701-4715 (2020)
Shandong University
Molecule Property Analyses of Active Compounds for
J Med Chem 63: 8917-8955 (2020)
Russian Academy Of Science
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
J Med Chem 63: 5242-5256 (2020)
University Of Texas Medical Branch
PTP1B-Inhibiting Branched-Chain Fatty Acid Dimers from
J Nat Prod 83: 1598-1610 (2020)
University Of Copenhagen
Advances in the Development of Phosphodiesterase-4 Inhibitors.
J Med Chem 63: 10594-10617 (2020)
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital
An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice.
Sci Transl Med 12: 1-15 (2020)
University Of North Carolina At Chapel Hill
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.
Bioorg Med Chem 28: (2020)
Pfizer
Identification of the Clinical Development Candidate
J Med Chem 63: 6679-6693 (2020)
Array Biopharma
Interrogating the Lactate Dehydrogenase Tetramerization Site Using (Stapled) Peptides.
J Med Chem 63: 4628-4643 (2020)
Universit£
S1P
Bioorg Med Chem Lett 30: (2020)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Identification of a new class of non-electrophilic TRPA1 agonists by a structure-based virtual screening approach.
Bioorg Med Chem Lett 30: (2020)
Kyoto University
In silico and in vitro studies on interaction of novel non-imidazole histamine H
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
J Med Chem 63: 4929-4956 (2020)
University Of Washington
Discovery of new LXR? agonists as glioblastoma inhibitors.
Eur J Med Chem 194: (2020)
Sun Yat-Sen University
Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.
Bioorg Med Chem 28: (2020)
Annamalai University
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.
Bioorg Med Chem 28: (2020)
Cracow University Of Technology
A chemically stable peptide agonist to neuromedin U receptor type 2.
Bioorg Med Chem 28: (2020)
Tokyo University Of Pharmacy And Life Sciences
Finding the mechanism of esterase D activation by a small molecule.
Bioorg Med Chem Lett 30: (2020)
Shandong University
Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase.
Bioorg Med Chem Lett 30: (2020)
Tongji University
Environment-sensitive fluorescent inhibitors of histone deacetylase.
Bioorg Med Chem Lett 30: (2020)
Shandong University
A potent photoreactive general anesthetic with novel binding site selectivity for GABA
Eur J Med Chem 194: (2020)
University Of Illinois At Chicago
New CDK8 inhibitors as potential anti-leukemic agents - Design, synthesis and biological evaluation.
Bioorg Med Chem 28: (2020)
Nord University
Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
J Med Chem 63: 4293-4305 (2020)
Dana-Farber Cancer Institute
New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A
Bioorg Med Chem Lett 30: (2020)
Universit£
Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
Eur J Med Chem 194: (2020)
Nanyang Normal University
Fragment-Based Design of
J Med Chem 63: 4749-4761 (2020)
University Of Cambridge
Furofuranone Lignans from
J Nat Prod 83: 1424-1431 (2020)
Universidad Aut£Noma Del Estado De Morelos
Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase.
Bioorg Med Chem 28: (2020)
University Of Iowa
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M
J Med Chem 63: 4133-4154 (2020)
University Of Regensburg
Rationally Designed Small-Molecule Inhibitors Targeting an Unconventional Pocket on the TLR8 Protein-Protein Interface.
J Med Chem 63: 4117-4132 (2020)
The University Of Tokyo
Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors.
Eur J Med Chem 194: (2020)
Shenyang Pharmaceutical University
Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.
J Med Chem 63: 3996-4004 (2020)
Ku Leuven
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
J Nat Prod 83: 1092-1098 (2020)
University Of Mississippi
Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors.
Eur J Med Chem 194: (2020)
College Of Pharmacy Of Liaoning University
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.
J Med Chem 63: 6513-6522 (2020)
Vanderbilt University School Of Medicine
Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design.
J Med Chem 63: 4315-4333 (2020)
Vanderbilt University
Discovery of Selective Small Molecule Degraders of BRAF-V600E.
J Med Chem 63: 4069-4080 (2020)
Cullgen
Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery.
J Med Chem 63: 3881-3895 (2020)
Dalian University Of Technology
Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity.
J Med Chem 63: 4306-4314 (2020)
University Of Florence
Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells.
Eur J Med Chem 194: (2020)
Sichuan University
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.
Bioorg Med Chem 28: (2020)
Fujian Medical University (Fmu)
N-benzyl 4,4-disubstituted piperidines as a potent class of influenza H1N1 virus inhibitors showing a novel mechanism of hemagglutinin fusion peptide interaction.
Eur J Med Chem 194: (2020)
Instituto De Qu£Mica M£Dica (C.S.I.C.)
Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide.
Eur J Med Chem 194: (2020)
Henan University
Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation.
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides.
J Med Chem 63: 4227-4255 (2020)
Wayne State University
Discovery of a Potent and Selective NF-?B-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo.
J Med Chem 63: 4388-4407 (2020)
Chinese Academy Of Sciences
Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73.
J Med Chem 63: 3935-3955 (2020)
Arcus Biosciences
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
J Med Chem 63: 4256-4292 (2020)
National Center For Advancing Translational Sciences
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
J Med Chem 63: 3915-3934 (2020)
Karolinska Institutet
Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX.
Bioorg Med Chem 28: (2020)
Jamia Millia Islamia
The signal peptide as a new target for drug design.
Bioorg Med Chem Lett 30: (2020)
University Of Nevada
Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation.
Bioorg Med Chem Lett 30: (2020)
Andhra University
2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment.
J Med Chem 63: 3908-3914 (2020)
Cha University
CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
J Med Chem 63: 4215-4226 (2020)
Zhejiang University
Discovery of 8-Methyl-pyrrolo[1,2-
J Med Chem 63: 3956-3975 (2020)
Chinese Academy Of Sciences
Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X.
Eur J Med Chem 193: (2020)
University Of Ljubljana
Small molecule inhibitors of I?B kinase ?: A chip-based screening and molecular docking simulation.
Bioorg Med Chem 28: (2020)
Kangwon National University
Anti-inflammatory effect and inhibition of nitric oxide production by targeting COXs and iNOS enzymes with the 1,2-diphenylbenzimidazole pharmacophore.
Bioorg Med Chem 28: (2020)
Instituto Polit£Cnico Nacional
Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
Eur J Med Chem 193: (2020)
Shenyang Pharmaceutical University
Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes.
Eur J Med Chem 193: (2020)
Kurukshetra University
Development of potent inhibitors of the human microsomal epoxide hydrolase.
Eur J Med Chem 193: (2020)
University Of California Davis
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.
J Med Chem 63: 4183-4204 (2020)
Japanese Foundation For Cancer Research
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.
J Med Chem 63: 4155-4170 (2020)
Glaxosmithkline
Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads.
J Med Chem 63: 4107-4116 (2020)
Bicycletx
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
J Med Chem 63: 4090-4106 (2020)
Chinese Academy Of Sciences
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.
J Med Chem 63: 4349-4369 (2020)
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
High throughput in vivo phenotypic screening for drug repurposing: Discovery of MLR-1023 a novel insulin sensitizer and novel Lyn kinase activator with clinical proof of concept.
Bioorg Med Chem 28: (2020)
Melior Discovery
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Liaocheng University
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.
Eur J Med Chem 193: (2020)
Shanghai Pharmaceuticals Holding
Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides.
Eur J Med Chem 193: (2020)
Beijing Institute Of Technology
Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions.
Eur J Med Chem 193: (2020)
Harbin Institute Of Technology
Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.
Bioorg Med Chem Lett 30: (2020)
Daiichi Sankyo
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
Bioorg Med Chem 28: (2020)
University Of Tennessee Health Science Center
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Bioorg Med Chem 28: (2020)
Lanzhou University
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.
Eur J Med Chem 193: (2020)
University Of Regensburg
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved ?-ketoamide inhibitors.
Science 368: 409-412 (2020)
University Of Lubeck
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.
Bioorg Med Chem 28: (2020)
University Of Messina
Prenylated Phenolic Compounds from the Aerial Parts of
J Nat Prod 83: 814-824 (2020)
Peking University
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and
J Med Chem 63: 3508-3521 (2020)
Istituto Italiano Di Tecnologia
Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds.
J Med Chem 63: 3485-3507 (2020)
University Of Antwerp
Discovery of cyclic guanidine-linked sulfonamides as inhibitors of LMTK3 kinase.
Bioorg Med Chem Lett 30: (2020)
San Diego State University
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
Bioorg Med Chem Lett 30: (2020)
Institute Of Technology
-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition.
J Med Chem 63: 7475-7490 (2020)
University Of California
LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease.
J Med Chem 63: 3763-3783 (2020)
University Of Kentucky
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
ACS Med Chem Lett 11: 385-392 (2020)
Duke University
Design and Optimization of 3'-(Imidazo[1,2-
ACS Med Chem Lett 11: 379-384 (2020)
Jinan University
Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.
ACS Med Chem Lett 11: 371-378 (2020)
University Of Pennsylvania
Development of a Versatile and Sensitive Direct Ligand Binding Assay for Human NR5A Nuclear Receptors.
ACS Med Chem Lett 11: 365-370 (2020)
Emory University
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
ACS Med Chem Lett 11: 358-364 (2020)
Gilead Sciences
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
ACS Med Chem Lett 11: 346-352 (2020)
Dana-Farber Cancer Institute
SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
ACS Med Chem Lett 11: 340-345 (2020)
University Of North Carolina At Chapel Hill (Unc-Ch)
An Alkyne-functionalized Arginine for Solid-Phase Synthesis Enabling "Bioorthogonal" Peptide Conjugation.
ACS Med Chem Lett 11: 334-339 (2020)
University Of Regensburg
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
ACS Med Chem Lett 11: 327-333 (2020)
Genentech
Regioisomeric Family of Novel Fluorescent Substrates for SHIP2.
ACS Med Chem Lett 11: 309-315 (2020)
School Of Biological Sciences, Uea
Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1
ACS Med Chem Lett 11: 303-308 (2020)
Division Of Janssen-Cilag
Design of Dual Inhibitors of Soluble Epoxide Hydrolase and LTA
ACS Med Chem Lett 11: 298-302 (2020)
Goethe University Frankfurt
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
ACS Med Chem Lett 11: 272-277 (2020)
University Of Minnesota
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
ACS Med Chem Lett 11: 266-271 (2020)
Bristol-Myers Squibb Research & Development
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.
Eur J Med Chem 193: (2020)
Fudan University
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.
Eur J Med Chem 193: (2020)
Lanzhou University
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds.
J Med Chem 63: 6315-6386 (2020)
Bristol Myers Squibb
Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance.
Eur J Med Chem 193: (2020)
Shanghaitech University
Synthesis and pharmacokinetic study of a
Bioorg Med Chem Lett 30: (2020)
Harvard Medical School
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.
J Med Chem 63: 3634-3664 (2020)
University Of Illinois At Chicago
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Bioorg Med Chem Lett 30: (2020)
Merck
Lead discovery, chemical optimization, and biological evaluation studies of novel histone methyltransferase SET7 small-molecule inhibitors.
Bioorg Med Chem Lett 30: (2020)
University Of Chinese Academy Of Sciences
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment.
Bioorg Med Chem Lett 30: (2020)
Jiangxi Science & Technology Normal University
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.
Bioorg Med Chem 28: (2020)
University Of Sharjah
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 30: (2020)
Changzhou University
Design and synthesis of selective degraders of EGFR
Eur J Med Chem 192: (2020)
Jinan University
Design, synthesis, and evaluation of N-phenyl-4-(2-phenylsulfonamido)-benzamides as microtubule-targeting agents in drug-resistant cancer cells, displaying HDAC inhibitory response.
Eur J Med Chem 192: (2020)
Taipei Medical University
Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists.
Eur J Med Chem 192: (2020)
China Pharmaceutical University
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.
Eur J Med Chem 192: (2020)
University Of Innsbruck
Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening.
Bioorg Med Chem Lett 30: (2020)
University Of The Western Cape
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A
Bioorg Med Chem Lett 30: (2020)
Universit£
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Eur J Med Chem 192: (2020)
Xihua University
Antiausterity Activity of Secondary Metabolites from the Roots of
J Nat Prod 83: 1099-1106 (2020)
University Of Innsbruck
Anti-inflammatory Metabolites from
J Nat Prod 83: 881-887 (2020)
Korea University
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.
J Med Chem 63: 3665-3677 (2020)
East China Normal University
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
J Med Chem 63: 3701-3712 (2020)
University Of Perugia
Investigation of Inactive-State ? Opioid Receptor Homodimerization via Single-Molecule Microscopy Using New Antagonistic Fluorescent Probes.
J Med Chem 63: 3596-3609 (2020)
Julius Maximilian University Of W£Rzburg
Discovery of pyrazole derivatives as cellular active inhibitors of histone lysine specific demethylase 5B (KDM5B/JARID1B).
Eur J Med Chem 192: (2020)
Zhengzhou University
Discovery of Thieno[2,3-
J Med Chem 63: 3678-3700 (2020)
Sichuan University And Collaborative Innovation Center Of Biotherapy
Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
Eur J Med Chem 192: (2020)
Taipei Medical University
Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
Eur J Med Chem 192: (2020)
Jiangsu Key Laboratory For Functional Substance Of Chinese Medicine
Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to
J Med Chem 63: 3047-3065 (2020)
Universit£
Bicyclic ?-Iminophosphonates as High Affinity Imidazoline I
J Med Chem 63: 3610-3633 (2020)
University Of Barcelona
Bioactive Azepine-Indole Alkaloids from
J Nat Prod 83: 852-863 (2020)
Universidade Federal Do Rio Grande Do Sul-Ufrgs
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.
J Med Chem 63: 7491-7507 (2020)
Qpex Biopharma
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?
J Med Chem 63: 7458-7474 (2020)
Lebanese American University
Synthesis of multimeric pyrrolidine iminosugar inhibitors of human ?-glucocerebrosidase and ?-galactosidase A: First example of a multivalent enzyme activity enhancer for Fabry disease.
Eur J Med Chem 192: (2020)
Universidad De Sevilla
Design and synthesis of tripeptidyl furylketones as selective inhibitors against the ?5 subunit of human 20S proteasome.
Eur J Med Chem 192: (2020)
Peking University Health Science Center
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.
Bioorg Med Chem 28: (2020)
Guizhou Medical University
Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
Eur J Med Chem 192: (2020)
The Research Institute Of The Mcgill University Health Center/Glen Hospital
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.
Bioorg Med Chem Lett 30: (2020)
Shandong Provincial Hospital Affiliated To Shandong University
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
J Med Chem 63: 3215-3226 (2020)
Takeda Pharmaceutical
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.
J Med Chem 63: 7957-7985 (2020)
Genentech
Distribution of Bibenzyls, Prenyl Bibenzyls, Bis-bibenzyls, and Terpenoids in the Liverwort Genus
J Nat Prod 83: 756-769 (2020)
Tokushima Bunri University
Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators.
J Med Chem 63: 3577-3595 (2020)
University Of Copenhagen
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Bioorg Med Chem Lett 30: (2020)
Jiangsu Aosaikang Pharmaceutical
Identification of Potent
J Med Chem 63: 3188-3204 (2020)
The University Of Tokyo
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
J Med Chem 63: 2915-2929 (2020)
Janssen Research And Development
Discovery and Development of Small-Molecule Inhibitors of Glycogen Synthase.
J Med Chem 63: 3538-3551 (2020)
Indiana University School Of Medicine
The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
Eur J Med Chem 192: (2020)
Nanyang Normal University
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.
J Med Chem 63: 6648-6676 (2020)
Celgene
Discovery and SARs of 5-Chloro-
J Med Chem 63: 3327-3347 (2020)
Anhui Medical University
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.
Bioorg Med Chem 28: (2020)
Assiut University
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.
J Med Chem 63: 3298-3316 (2020)
Texas A&M University
Calorimetric Studies of Binary and Ternary Molecular Interactions between Transthyretin, A? Peptides, and Small-Molecule Chaperones toward an Alternative Strategy for Alzheimer's Disease Drug Discovery.
J Med Chem 63: 3205-3214 (2020)
Institut De Qu??Mica Avan£Ada De Catalunya (I.Q.A.C.-C.S.I.C.)
Design and synthesis of dansyl-labeled inhibitors of steroid sulfatase for optical imaging.
Bioorg Med Chem 28: (2020)
Chu De Qu£Bec - Research Center
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.
Bioorg Med Chem Lett 30: (2020)
East China University Of Science & Technology
Design and synthesis of potent PAR-1 antagonists based on vorapaxar.
Bioorg Med Chem Lett 30: (2020)
Hebei University Of Technology
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
Bioorg Med Chem Lett 30: (2020)
University Of Chinese Academy Of Sciences
Substituted 1-methyl-4-phenylpyrrolidin-2-ones - Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors.
Eur J Med Chem 191: (2020)
Monash University (Parkville Campus)
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
J Med Chem 63: 4655-4684 (2020)
Monash University (Parkville Campus)
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
J Med Chem 63: 3370-3380 (2020)
Guangzhou University Of Chinese Medicine
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.
Eur J Med Chem 192: (2020)
Zhejiang University
Discovery of sulfonamides and 9-oxo-2,8-diazaspiro[5,5]undecane-2-carboxamides as human kynurenine aminotransferase 2 (KAT2) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Orion Pharma
Discovery of 4-((1-(1H-imidazol-2-yl)alkoxy)methyl)pyridines as a new class of Trypanosoma cruzi growth inhibitors.
Bioorg Med Chem Lett 30: (2020)
Irbm
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.
Eur J Med Chem 192: (2020)
China Pharmaceutical University
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
J Med Chem 63: 3348-3358 (2020)
Glaxosmithkline
Identification of C10 nitrogen-containing aporphines with dopamine D
Bioorg Med Chem Lett 30: (2020)
City University Of New York
The discovery, design and synthesis of potent agonists of adenylyl cyclase type 2 by virtual screening combining biological evaluation.
Eur J Med Chem 191: (2020)
Chinese Academy Of Sciences
Novel pyrrolidinone derivative lacks claimed histamine H
Eur J Med Chem 191: (2020)
Heinrich Heine University D£Sseldorf
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
Eur J Med Chem 191: (2020)
Jagiellonian University Medical College
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).
Eur J Med Chem 191: (2020)
University Of Regensburg
Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors.
J Med Chem 63: 2894-2914 (2020)
Monash University
Substituent Position of Iminocyclitols Determines the Potency and Selectivity for Gut Microbial Xenobiotic-Reactivating Enzymes.
J Med Chem 63: 4617-4627 (2020)
Academia Sinica
Dimerization of ?-Conotoxins as a Strategy to Enhance the Inhibition of the Human ?7 and ?9?10 Nicotinic Acetylcholine Receptors.
J Med Chem 63: 2974-2985 (2020)
Ocean University Of China
Diterpenoids from the Root Bark of
J Nat Prod 83: 1229-1237 (2020)
Chinese Academy Of Sciences
One-pot synthesis of thioxo-tetrahydropyrimidine derivatives as potent ?-glucuronidase inhibitor, biological evaluation, molecular docking and molecular dynamics studies.
Bioorg Med Chem 28: (2020)
Shiraz University Of Medical Sciences
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
Eur J Med Chem 191: (2020)
China Pharmaceutical University
Novel ?- and ?-Amino Acid-Derived Inhibitors of Prostate-Specific Membrane Antigen.
J Med Chem 63: 3261-3273 (2020)
Korea University
Effective Application of Metabolite Profiling in Drug Design and Discovery.
J Med Chem 63: 6387-6406 (2020)
Pfizer
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPAR? Agonists as Leads for Retinal Disorders.
J Med Chem 63: 2854-2876 (2020)
University Of Oklahoma
Novel cilengitide-based cyclic RGD peptides as ?v?
Bioorg Med Chem Lett 30: (2020)
Division Of Organic Chemistry Csir-National Chemical Laboratory (Ncl)
Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
Eur J Med Chem 191: (2020)
University Of Szeged
Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains.
J Med Chem 63: 3227-3237 (2020)
Moffitt Cancer Center
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
DNA sequence-specific ligands. XVIII. Synthesis, physico-chemical properties; genetic, virological, and biochemical studies of fluorescent dimeric bisbenzimidazoles DBPA(n).
Bioorg Med Chem 28: (2020)
Russian Academy Of Sciences
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
Bioorg Med Chem 28: (2020)
Guizhou Medical University
Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.
Eur J Med Chem 191: (2020)
Southwest Jiaotong University
Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.
Eur J Med Chem 191: (2020)
University Of Tabriz
Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Hefei University Of Technology
Discovery of novel hydroxyamidine derivatives as indoleamine 2,3-dioxygenase 1 inhibitors with in vivo anti-tumor efficacy.
Bioorg Med Chem Lett 30: (2020)
Fudan University
Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor.
Bioorg Med Chem 28: (2020)
Takeda Pharmaceutical
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Eur J Med Chem 191: (2020)
Huazhong University Of Science And Technology
Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential.
Eur J Med Chem 191: (2020)
University Of Belgrade
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer.
Bioorg Med Chem Lett 30: (2020)
University Of Sussex
Synthesis, biological evaluation and molecular modeling study of [1,2,4]-Triazolo[4,3-c]quinazolines: New class of EGFR-TK inhibitors.
Bioorg Med Chem 28: (2020)
Mansoura University
Discovery of 4,6-
J Med Chem 63: 2877-2893 (2020)
Hubei University Of Technology
Isolation and Structural Characterization of Specific Bacterial ?-Glucuronidase Inhibitors from Noni (
J Nat Prod 83: 825-833 (2020)
Wayne State University
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
J Med Chem 63: 5102-5118 (2020)
TBA
Design, synthesis and identification of N, N-dibenzylcinnamamide (DBC) derivatives as novel ligands for ?-synuclein fibrils by SPR evaluation system.
Bioorg Med Chem 28: (2020)
Fudan University
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
J Med Chem 63: 2620-2637 (2020)
Bristol-Myers Squibb Research And Development
Structurally novel PI3K?/? dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.
Eur J Med Chem 191: (2020)
Anhui University Of Chinese Medicine
Inhibition of striatal-enriched protein tyrosine phosphatase by targeting computationally revealed cryptic pockets.
Eur J Med Chem 190: (2020)
Shandong University
Targeting different binding sites in the CFTR structures allows to synergistically potentiate channel activity.
Eur J Med Chem 190: (2020)
Universit£
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.
J Nat Prod 83: 461-467 (2020)
Usona Institute
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
J Med Chem 63: 2958-2973 (2020)
Genomics Institute Of The Novartis Research Foundation (Gnf)
Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases
J Med Chem 63: 5697-5722 (2020)
Novartis Institutes For Biomedical Research
DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors.
J Med Chem 63: 3552-3562 (2020)
Glaxosmithkline
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
ACS Med Chem Lett 11: 188-194 (2020)
Novartis Institutes For Biomedical Research
Discovery of Hydroxyamidine Based Inhibitors of IDO1 for Cancer Immunotherapy with Reduced Potential for Glucuronidation.
ACS Med Chem Lett 11: 179-187 (2020)
Phenex Pharmaceuticals
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.
ACS Med Chem Lett 11: 172-178 (2020)
Bristol-Myers Squibb Research & Development
Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.
ACS Med Chem Lett 11: 166-171 (2020)
Korea Research Institute Of Chemical Technology
Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.
ACS Med Chem Lett 11: 141-146 (2020)
Baylor University
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
ACS Med Chem Lett 11: 133-140 (2020)
Glaxosmithkline
Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity.
ACS Med Chem Lett 11: 127-132 (2020)
University Of California
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR??t Allosteric Inhibitors for Autoimmune Diseases
ACS Med Chem Lett 11: 114-119 (2020)
Merck
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
ACS Med Chem Lett 11: 101-107 (2020)
Agios Pharmaceuticals
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.
Eur J Med Chem 190: (2020)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Serendipitous Discovery of Leucine and Methionine Depletion Agents during the Search for Polyamine Transport Inhibitors.
J Med Chem 63: 2814-2832 (2020)
University Of Central Florida
Design, Synthesis, and Biological Evaluation of Imidazo[1,2-
J Med Chem 63: 3028-3046 (2020)
East China Normal University
Optimization of 4-Aminopiperidines as Inhibitors of Influenza A Viral Entry That Are Synergistic with Oseltamivir.
J Med Chem 63: 3120-3130 (2020)
University Of Illinois At Chicago
Dual Binding to Orthosteric and Allosteric Sites Enhances the Anticancer Activity of a TRAP1-Targeting Drug.
J Med Chem 63: 2930-2940 (2020)
Ulsan National Institutes Of Science And Technology (Unist)
A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring N
Bioorg Med Chem 28: (2020)
Fudan University
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
Bioorg Med Chem Lett 30: (2020)
University Of Pennsylvania
Design, synthesis and evaluation of unnatural peptides as T1R2/T1R3 PAMs.
Bioorg Med Chem Lett 30: (2020)
Ajinomoto
Recent advances in TRPV4 agonists and antagonists.
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.
Bioorg Med Chem Lett 30: (2020)
Merck
Unexpected small molecules as novel SIRT2 suicide inhibitors.
Bioorg Med Chem 28: (2020)
Engineering Research Center For The Development And Application Of Ethnic Medicine And Tcm (Ministry Of Education)
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
Bioorg Med Chem 28: (2020)
Georgia Institute Of Technology
Yanhusanines A-F, Isoquinoline-Derived Alkaloid Enantiomers from
J Nat Prod 83: 489-496 (2020)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.
J Med Chem 63: 6600-6623 (2020)
Biohaven Pharmaceuticals
Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition.
Eur J Med Chem 190: (2020)
The Key Laboratory Of Chemistry For Natural Products Of Guizhou Province And Chinese Academy Of Sciences
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
Eur J Med Chem 190: (2020)
Taipei Medical University
Design, synthesis and biological activity of N
Eur J Med Chem 190: (2020)
Peking University
Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors.
Bioorg Med Chem Lett 30: (2020)
Xiamen University
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand.
Bioorg Med Chem Lett 30: (2020)
Jinzhou Medical University
Novel, Self-Assembling Dimeric Inhibitors of Human ? Tryptase.
J Med Chem 63: 3004-3027 (2020)
Weill Cornell Medicine
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.
Bioorg Med Chem 28: (2020)
Nyrada
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
J Med Chem 63: 3252-3260 (2020)
University Of Oxford
The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology.
J Med Chem 63: 6624-6647 (2020)
University Of Perugia
Discovery of disubstituted xylylene derivatives as small molecule direct inhibitors of Keap1-Nrf2 protein-protein interaction.
Bioorg Med Chem 28: (2020)
The State University Of New Jersey
Discovery and structure-activity relationships of spiroindolines as novel inducers of oligodendrocyte progenitor cell differentiation.
Bioorg Med Chem 28: (2020)
Asubio Pharma
Discovery of 2-aminoisobutyric acid ethyl ester (AIBEE) phosphoramidate prodrugs for delivering nucleoside HCV NS5B polymerase inhibitors.
Bioorg Med Chem Lett 30: (2020)
Abbvie
2-Substituted ?,?-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.
J Med Chem 63: 2941-2957 (2020)
University Of Bonn
Inclusion of a 5-fluorouracil moiety in nitrogenous bases derivatives as human carbonic anhydrase IX and XII inhibitors produced a targeted action against MDA-MB-231 and T47D breast cancer cells.
Eur J Med Chem 190: (2020)
University Of Florence
STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae.
Bioorg Med Chem 28: (2020)
Kindai University
An increase in side-group hydrophobicity largely improves the potency of ritonavir-like inhibitors of CYP3A4.
Bioorg Med Chem 28: (2020)
University Of California
DNA-Encoded Library Screening as Core Platform Technology in Drug Discovery: Its Synthetic Method Development and Applications in DEL Synthesis.
J Med Chem 63: 6578-6599 (2020)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol
ACS Med Chem Lett 10: 1573-1578 (2019)
Lieber Institute For Brain Development
Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib.
J Med Chem 63: 2588-2619 (2020)
Istituto Italiano Di Tecnologia
Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors.
Bioorg Med Chem 28: (2020)
Lanzhou University
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
Bioorg Med Chem Lett 30: (2020)
Universit£
Inhibition of cholesteryl ester synthesis by polyacetylenes from Atractylodes rhizome.
Bioorg Med Chem Lett 30: (2020)
Kitasato University
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb Research And Development
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.
J Med Chem 63: 1724-1749 (2020)
Lindsley F. Kimball Research Institute
Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers
J Med Chem 63: 3104-3119 (2020)
Sichuan University
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.
J Med Chem 63: 3317-3326 (2020)
University Of Wollongong
Antimycobacterial Rufomycin Analogues from
J Nat Prod 83: 657-667 (2020)
University Of Illinois At Chicago
Acetylene Group, Friend or Foe in Medicinal Chemistry.
J Med Chem 63: 5625-5663 (2020)
St. John'S University
The Other Angiotensin II Receptor: AT
J Med Chem 63: 1978-1995 (2020)
Centre Hospitalier Universitaire Vaudois (Chuv) And University Of Lausanne (Unil
Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective.
J Med Chem 63: 1937-1963 (2020)
University Of Chemistry And Technology Prague
Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs).
J Med Chem 63: 5664-5674 (2020)
National Institute Of Chemistry
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine ?4?2 Receptor Antagonist for the Treatment of Depression.
J Med Chem 63: 2833-2853 (2020)
Suven Life Sciences
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS
J Med Chem 63: 4468-4483 (2020)
Astrazeneca
Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist.
J Med Chem 63: 5089-5099 (2020)
Chugai Pharmaceutical
BET proteins: Investigating BRDT as a potential target for male contraception.
Bioorg Med Chem Lett 30: (2020)
University Of Minnesota
Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.
Eur J Med Chem 190: (2020)
Consejo Superior De Investigaciones Cient�Ficas (Iqm-Csic)
Structural features and functional activities of benzimidazoles as NOD2 antagonists.
Eur J Med Chem 190: (2020)
University Of Ljubljana
Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma.
Eur J Med Chem 190: (2020)
China Pharmaceutical University
Design, synthesis and biological evaluation of 1-alkyl-5/6-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors.
Eur J Med Chem 190: (2020)
Shenyang Pharmaceutical University
Protein-Induced Change in Ligand Protonation during Trypsin and Thrombin Binding: Hint on Differences in Selectivity Determinants of Both Proteins?
J Med Chem 63: 3274-3289 (2020)
Philipps-University Marburg
Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 30: (2020)
Hebei University
Anti-diabetic drugs recent approaches and advancements.
Bioorg Med Chem 28: (2020)
Mizoram University
Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
Bioorg Med Chem 28: (2020)
Jinan University
Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
Eur J Med Chem 189: (2020)
Sichuan University
New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies.
Bioorg Med Chem 28: (2020)
National Research Centre
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR?t.
Bioorg Med Chem Lett 30: (2020)
Reata Pharmaceuticals
Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine.
Eur J Med Chem 189: (2020)
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer
Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis.
J Med Chem 63: 1576-1596 (2020)
Czech Academy Of Sciences
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human ?-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.
J Med Chem 63: 2986-3003 (2020)
Icahn School Of Medicine At Mount Sinai
Discovery of thieno[2,3-d]pyrimidin-4(3H)-one derivatives as a new class of ROCK inhibitors.
Bioorg Med Chem Lett 30: (2020)
Sichuan University
Optimization of 8-oxoadenines with toll-like-receptor 7 and 8 activity.
Bioorg Med Chem Lett 30: (2020)
University Of Montana
Synthesis and evaluation of novel radioiodinated PSMA targeting ligands for potential radiotherapy of prostate cancer.
Bioorg Med Chem 28: (2020)
Beijing Normal University
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.
Bioorg Med Chem 28: (2020)
University Of Strathclyde
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