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Discovery of New Imidazo[2,1-
J Med Chem 64: 6877-6901 (2021)
National Research Centre (Nrc)
Novel Mixed NOP/Opioid Receptor Peptide Agonists.
J Med Chem 64: 6656-6669 (2021)
University Of Ferrara
Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy.
Eur J Med Chem 221: (2021)
Tehran University Of Medical Sciences
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.
Eur J Med Chem 221: (2021)
Shandong University
Computer-aided design of 1,4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases.
Bioorg Med Chem 41: (2021)
Federal University Of Alagoas
A novel GSK-3 inhibitor binds to GSK-3? via a reversible, time and Cys-199-dependent mechanism.
Bioorg Med Chem 40: (2021)
Ohio University
Nitrile-based peptoids as cysteine protease inhibitors.
Bioorg Med Chem 41: (2021)
University Of S£O Paulo
Green synthesis of therapeutically active 1,3,4-oxadiazoles as antioxidants, selective COX-2 inhibitors and their in silico studies.
Bioorg Med Chem Lett 43: (2021)
Karnatak University
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Bioorg Med Chem Lett 47: (2021)
Glaxosmithkline
Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study.
Bioorg Med Chem Lett 44: (2021)
Nankai University
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Bioorg Med Chem Lett 44: (2021)
Merck
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.
Bioorg Med Chem Lett 44: (2021)
Bristol Myers Squibb Research And Development
Synthesis and Evaluation of PPAR? Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
J Med Chem 64: 6996-7032 (2021)
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin-3 Inhibitors.
J Med Chem 64: 6634-6655 (2021)
Bristol Myers Squibb
Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors.
Bioorg Med Chem Lett 44: (2021)
Roche Innovation Center Shanghai
Promising anti-SARS-CoV-2 drugs by effective dual targeting against the viral and host proteases.
Bioorg Med Chem Lett 43: (2021)
Bristol University
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
Bioorg Med Chem Lett 43: (2021)
University Hospital Hradec Kralove
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.
J Med Chem 64: 10682-10710 (2021)
Goethe University Frankfurt Am Main
Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.
Bioorg Med Chem 40: (2021)
Agri Ibrahim Cecen University
Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
Bioorg Med Chem 40: (2021)
Shandong University
Dual-Targeting Antiproliferation Hybrids Derived from 1-Deoxynojirimycin and Kaempferol Induce MCF-7 Cell Apoptosis through the Mitochondria-Mediated Pathway.
J Nat Prod 84: 1534-1543 (2021)
Jiangsu University Of Science And Technology
Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
J Med Chem 64: 6745-6764 (2021)
Servier Research Institute Of Medicinal Chemistry
Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold.
Eur J Med Chem 220: (2021)
University Of Pisa
Structure-Guided Design of the First Noncovalent Small-Molecule Inhibitor of CRM1.
J Med Chem 64: 6596-6607 (2021)
Sichuan University And Collaborative Innovation Centre Of Biotherapy
Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation.
J Med Chem 64: 6802-6813 (2021)
Ecole Polytechnique F�D�Rale De Lausanne (Epfl)
Design and Synthesis of Highly Selective Brain Penetrant p38? Mitogen-Activated Protein Kinase Inhibitors.
J Med Chem 65: 1225-1242 (2022)
Eberhard Karls Universit£T T£Bingen
Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection.
J Med Chem 64: 6856-6876 (2021)
China Pharmaceutical University
Design, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors.
Bioorg Med Chem 40: (2021)
China Pharmaceutical University
Exploiting the HSP60/10 chaperonin system as a chemotherapeutic target for colorectal cancer.
Bioorg Med Chem 40: (2021)
Indiana University School Of Medicine
Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma.
Bioorg Med Chem 40: (2021)
Nanjing Normal University
Kinase Inhibitors as Underexplored Antiviral Agents.
J Med Chem 65: 935-954 (2022)
Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)
Adamantane derivatives as potential inhibitors of p37 major envelope protein and poxvirus reproduction. Design, synthesis and antiviral activity.
Eur J Med Chem 221: (2021)
Samara State Technical University
Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies.
Eur J Med Chem 221: (2021)
Egyptian Russian University
Novel hybrid conjugates with dual estrogen receptor ? degradation and histone deacetylase inhibitory activities for breast cancer therapy.
Bioorg Med Chem 40: (2021)
Wuhan University
Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells.
Bioorg Med Chem 40: (2021)
Shanghai University Of Traditional Chinese Medicine
Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability.
Bioorg Med Chem Lett 43: (2021)
Vrije Universiteit Brussel
Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
Eur J Med Chem 221: (2021)
Shandong University
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.
Bioorg Med Chem Lett 43: (2021)
Ningxia Medical University
Folate-targeted verrucarin A reduces the number of activated macrophages in a mouse model of acute peritonitis.
Bioorg Med Chem Lett 42: (2021)
Indian Institute Of Technology Indore
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors.
Eur J Med Chem 221: (2021)
University Of Perugia
Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition.
Bioorg Med Chem 40: (2021)
South Valley University
Halting the Spread of Herpes Simplex Virus-1: The Discovery of an Effective Dual ?v?6/?v?8 Integrin Ligand.
J Med Chem 64: 6972-6984 (2021)
Universit£
Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation.
Eur J Med Chem 220: (2021)
University Of Chinese Academy Of Sciences
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
Eur J Med Chem 220: (2021)
Xinxiang Medical University
Cryptic Biosynthesis of the Berkeleypenostatins from Coculture of Extremophilic
J Nat Prod 84: 1656-1665 (2021)
TBA
Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1? Axis.
J Nat Prod 84: 1563-1572 (2021)
University Of Rhode Island
Discovery of Novel, Potent Inhibitors of Hydroxy Acid Oxidase 1 (HAO1) Using DNA-Encoded Chemical Library Screening.
J Med Chem 64: 6730-6744 (2021)
X-Chem
Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents.
Bioorg Med Chem Lett 43: (2021)
University Of North Carolina At Chapel Hill
Neuroactive Type-A ?-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk,
J Med Chem 64: 7033-7043 (2021)
University Of Utah
Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation.
J Med Chem 64: 5667-5688 (2021)
Sorbonne Universit£
Macrocyclic Peptides that Selectively Inhibit the
J Med Chem 64: 6262-6272 (2021)
Weill Cornell Medicine
Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.
Eur J Med Chem 220: (2021)
Shenyang Pharmaceutical University
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Eur J Med Chem 221: (2021)
Harvard Medical School
Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M.
J Med Chem 64: 5850-5862 (2021)
University Of Kentucky
Efficient Dimerization Disruption of
J Med Chem 64: 6137-6160 (2021)
Instituto De Qu£Mica M£Dica (Iqm-Csic)
From the Design to the
J Med Chem 64: 5429-5446 (2021)
Unitat Associada Al Csic
X-ray Crystal Structure-Guided Design and Optimization of 7
J Med Chem 64: 6985-6995 (2021)
Yonsei University
Discovery of cytotoxic natural products from Red Sea sponges: Structure and synthesis.
Eur J Med Chem 220: (2021)
Csir-National Institute Of Oceanography
Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.
Eur J Med Chem 220: (2021)
Sichuan University
Synthesis, biological, and photophysical studies of molecular rotor-based fluorescent inhibitors of the trypanosome alternative oxidase.
Eur J Med Chem 220: (2021)
Instituto De Qu£Mica M£Dica
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
J Med Chem 64: 6037-6058 (2021)
Galapagos
Discovery of Potent Coumarin-Based Kinetic Stabilizers of Amyloidogenic Immunoglobulin Light Chains Using Structure-Based Design.
J Med Chem 64: 6273-6299 (2021)
The Scripps Research Institute
Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- and BCRP-Mediated Multidrug Resistance.
J Med Chem 64: 6179-6197 (2021)
China Pharmaceutical University
Discovery of 4-Arylindolines Containing a Thiazole Moiety as Potential Antitumor Agents Inhibiting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction.
J Med Chem 64: 5519-5534 (2021)
Shenyang Pharmaceutical University
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.
Eur J Med Chem 219: (2021)
Taipei Medical University
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
Eur J Med Chem 220: (2021)
Chinese Academy Of Medical Science And Peking Union Medical College
A ?-lactam siderophore antibiotic effective against multidrug-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter spp.
Eur J Med Chem 220: (2021)
Louis Stokes Cleveland Department Of Veterans Affairs Medical Center
Rational modification, synthesis and biological evaluation of N-substituted phthalazinone derivatives designed to target interleukine-15 protein.
Bioorg Med Chem 39: (2021)
Universit£
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Bioorg Med Chem 40: (2021)
Emd Serono Research & Development Institute
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.
Bioorg Med Chem Lett 43: (2021)
Bristol-Myers Squibb
Discovery of a potent and selective Axl inhibitor in preclinical model.
Bioorg Med Chem 39: (2021)
Eisai
Design, synthesis of novel celastrol derivatives and study on their antitumor growth through HIF-1? pathway.
Eur J Med Chem 220: (2021)
Yanbian University
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.
J Med Chem 64: 5816-5837 (2021)
Shanghai Institute Of Materia Medica
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
J Med Chem 64: 6329-6357 (2021)
Novartis Institutes For Biomedical Research
Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists.
Eur J Med Chem 220: (2021)
Karlsruhe Institute Of Technology (Kit)
Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.
J Med Chem 64: 5645-5653 (2021)
University Of California
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
J Med Chem 64: 5730-5745 (2021)
Csic
Design of Dimeric Bile Acid Derivatives as Potent and Selective Human NTCP Inhibitors.
J Med Chem 64: 5973-6007 (2021)
National Institute Of Biological Sciences
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.
Eur J Med Chem 220: (2021)
Chinese Academy Of Medical Science And Peking Union Medical College
Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors.
Eur J Med Chem 220: (2021)
China Pharmaceutical University
A novel Hsp70 inhibitor specifically targeting the cancer-related Hsp70-Bim protein-protein interaction.
Eur J Med Chem 220: (2021)
Dalian University Of Technology
Developments of small molecules as inhibitors for carbonic anhydrase isoforms.
Bioorg Med Chem 39: (2021)
Georgia State University
Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site.
J Med Chem 64: 5766-5786 (2021)
University Of Innsbruck
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
J Med Chem 64: 5905-5930 (2021)
University Of Dundee
Discovery of 2-(3-(3-Carbamoylpiperidin-1-yl)phenoxy)acetic Acid Derivatives as Novel Small-Molecule Inhibitors of the ?-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.
J Med Chem 64: 5886-5904 (2021)
H. Lee Moffitt Cancer Center And Research Institute
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human ?7 Nicotinic Acetylcholine Receptors.
J Med Chem 64: 5620-5631 (2021)
Hainan University
Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
Eur J Med Chem 220: (2021)
India
Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy.
Eur J Med Chem 220: (2021)
Alexandria University
Chemoenzymatic synthesis of 2,6-disubstituted tetrahydropyrans with high ?
Eur J Med Chem 219: (2021)
Westf£Lische Wilhelms-Universit£T M£Nster
Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay.
Bioorg Med Chem 39: (2021)
University Of Auckland
Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing.
Bioorg Med Chem Lett 42: (2021)
National Institute Of Pharmaceutical Education And Research-Ahmedabad
Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective
J Med Chem 64: 5956-5972 (2021)
Northeastern University
Fragment-Based Design of a Potent MAT2a Inhibitor and
J Med Chem 64: 6814-6826 (2021)
Astrazeneca
Discovery of a Vitamin D Receptor-Silent Vitamin D Derivative That Impairs Sterol Regulatory Element-Binding Protein In Vivo.
J Med Chem 64: 5689-5709 (2021)
Teikyo University
Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains.
RSC Med Chem 12: 410-415 (2021)
University Of New South Wales
Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.
Bioorg Med Chem Lett 43: (2021)
University Of Nebraska Medical Center
Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
Bioorg Med Chem Lett 43: (2021)
Hibercell
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment.
Eur J Med Chem 220: (2021)
Shenyang Pharmaceutical University
Discovery of selective fragment-sized immunoproteasome inhibitors.
Eur J Med Chem 219: (2021)
Hungarian Academy Of Sciences
SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.
Bioorg Med Chem 39: (2021)
Taussig Cancer Institute
Design, synthesis and molecular docking studies of thymol based 1,2,3-triazole hybrids as thymidylate synthase inhibitors and apoptosis inducers against breast cancer cells.
Bioorg Med Chem 38: (2021)
Albaha University
Progress in developing MNK inhibitors.
Eur J Med Chem 219: (2021)
Ocean University Of China And Laboratory For Marine Drugs And Bioproducts
A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders.
Eur J Med Chem 219: (2021)
Dana-Farber Cancer Institute
Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.
Eur J Med Chem 219: (2021)
University Hospital Hradec Kralove
Novel 1,2,4-triazine-quinoline hybrids: The privileged scaffolds as potent multi-target inhibitors of LPS-induced inflammatory response via dual COX-2 and 15-LOX inhibition.
Eur J Med Chem 219: (2021)
Zagazig University
Identification of an allosteric and Smad3-selective inhibitor of p38?MAPK using a substrate-based approach.
Bioorg Med Chem Lett 43: (2021)
Carna Biosciences
Xanthine-Guanine-Hypoxanthine Phosphoribosyltransferase-A Putative Target for Drug Discovery against Gastrointestinal Tract Infections.
J Med Chem 64: 5710-5729 (2021)
The University Of Queensland
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.
J Med Chem 65: 2848-2865 (2022)
The University Of Arizona
From High-Throughput Screening to Target Validation: Benzo[
J Med Chem 64: 5931-5955 (2021)
Aptuit, An Evotec
Synthesis, Molecular Pharmacology, and Structure-Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists.
J Med Chem 64: 6381-6396 (2021)
West Virginia University
Discovery of Novel Pyrimidine-Based Capsid Assembly Modulators as Potent Anti-HBV Agents.
J Med Chem 64: 5500-5518 (2021)
Gwangju Institute Of Science And Technology (Gist)
Nucleotide analogues containing a pyrrolidine, piperidine or piperazine ring: Synthesis and evaluation of inhibition of plasmodial and human 6-oxopurine phosphoribosyltransferases and in vitro antimalarial activity.
Eur J Med Chem 219: (2021)
The Institute Of Organic Chemistry And Biochemistry Of The Czech Academy Of Sciences
Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
Bioorg Med Chem Lett 43: (2021)
Hefei University Of Technology
Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.
Bioorg Med Chem Lett 42: (2021)
The Institute Of Cancer Research
Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.
Bioorg Med Chem Lett 43: (2021)
Daiichi Sankyo
Positional Isomeric Effects on the Optical Properties, Multivalent Glycosidase Inhibition Effect, and Hypoglycemic Effect of Perylene Bisimide-deoxynojirimycin Conjugates.
J Med Chem 64: 5863-5873 (2021)
Hebei University
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
J Med Chem 64: 5577-5592 (2021)
University Of Minnesota
New tetrahydroisoquinoline-based D
Bioorg Med Chem Lett 42: (2021)
City University Of New York
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
J Med Chem 64: 6085-6136 (2021)
Medicines For Malaria Venture
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.
J Med Chem 64: 7331-7340 (2021)
TBA
Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1.
J Med Chem 64: 5838-5849 (2021)
Max Planck Institute Of Molecular Physiology
AAA ATPases as therapeutic targets: Structure, functions, and small-molecule inhibitors.
Eur J Med Chem 219: (2021)
California Institute Of Technology
Amphiphilic peptide-based MMP3 inhibitors for intra-articular treatment of knee OA.
Bioorg Med Chem 38: (2021)
Fidia Farmaceutici
Development of Dimethylisoxazole-Attached Imidazo[1,2-
J Med Chem 64: 5787-5801 (2021)
University Of Massachusetts Boston
Taurultams incorporating arylsulfonamide: First in vitro inhibition studies of ?-, ?- and ?-class Carbonic Anhydrases from Vibrio cholerae and Burkholderia pseudomallei.
Eur J Med Chem 219: (2021)
Ege University
Dipeptide inhibitors of the prostate specific membrane antigen (PSMA): A comparison of urea and thiourea derivatives.
Bioorg Med Chem Lett 42: (2021)
King'S College London
Discovery of a new series of PI3K-? inhibitors from Virtual Screening.
Bioorg Med Chem Lett 42: (2021)
Merck
Magnolol, a natural aldehyde dehydrogenase-2 agonist, inhibits the proliferation and collagen synthesis of cardiac fibroblasts.
Bioorg Med Chem Lett 43: (2021)
Southern Medical University
Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
Eur J Med Chem 219: (2021)
School Of Traditional Chinese Pharmacy
Azetidinimines as a novel series of non-covalent broad-spectrum inhibitors of ?-lactamases with submicromolar activities against carbapenemases KPC-2 (class A), NDM-1 (class B) and OXA-48 (class D).
Eur J Med Chem 219: (2021)
Universit£
Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.
Eur J Med Chem 219: (2021)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre
Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries.
Eur J Med Chem 219: (2021)
University Of Wisconsin-Madison
Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2.
Bioorg Med Chem 38: (2021)
University Of New South Wales (Unsw)
Dipyridyl-substituted thiosemicarbazone as a potent broad-spectrum inhibitor of metallo-?-lactamases.
Bioorg Med Chem 38: (2021)
Northwest University
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.
Bioorg Med Chem 39: (2021)
China Pharmaceutical University
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
J Med Chem 64: 6209-6220 (2021)
University Of Porto
First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.
J Med Chem 64: 9875-9890 (2021)
Takeda California
Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship,
J Med Chem 64: 6008-6020 (2021)
Northeastern University
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.
ACS Med Chem Lett 12: 653-661 (2021)
Merck
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
ACS Med Chem Lett 12: 647-652 (2021)
Jinan University
A Set of Highly Sensitive Sirtuin Fluorescence Probes for Screening Small-Molecular Sirtuin Defatty-Acylase Inhibitors.
ACS Med Chem Lett 12: 617-624 (2021)
Nagoya City University
Discovery of the First Orally Available, Selective K
ACS Med Chem Lett 12: 593-602 (2021)
Praxis Precision Medicines
Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity.
ACS Med Chem Lett 12: 572-578 (2021)
The University Of Tennessee Health Science Center
Novel Pyrimidine-5-carboxamide Compounds as NNMT Inhibitors for Treating Diabetes.
ACS Med Chem Lett 12: 538-539 (2021)
Smith, Gambrell & Russell
Heterocyclic Compounds as Monoacylglycerol Lipase (MAGL) Inhibitors.
ACS Med Chem Lett 12: 536-537 (2021)
Smith, Gambrell & Russell
Thienopyridinyl and Thiazolopyridinyl Compounds as IRAK4 Inhibitors.
ACS Med Chem Lett 12: 532-533 (2021)
Smith, Gambrell & Russell
Novel N-Heteroaryl Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.
ACS Med Chem Lett 12: 530-531 (2021)
Smith, Gambrell & Russell
Novel Pyridazines as Autotaxin Inhibitors for Treating Inflammatory Airway or Fibrotic Diseases.
ACS Med Chem Lett 12: 528-529 (2021)
Smith, Gambrell & Russell
Novel Azaquinolones as PARP1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 12: 524-525 (2021)
Smith, Gambrell & Russell
Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome.
Bioorg Med Chem 38: (2021)
South China Agricultural University
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.
Eur J Med Chem 219: (2021)
Sichuan University
Development of Potent NEDD8-Activating Enzyme Inhibitors Bearing a Pyrimidotriazole Scaffold.
J Med Chem 64: 6161-6178 (2021)
Shanghai Institute Of Materia Medica (Simm)
Covalent Occlusion of the ROR?t Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site.
ACS Med Chem Lett 12: 631-639 (2021)
Technische Universiteit Eindhoven
Synthesis, Inhibitory Activity, and
ACS Med Chem Lett 12: 610-616 (2021)
Czech Academy Of Sciences
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
ACS Med Chem Lett 12: 540-547 (2021)
Merck
Defining Target Engagement Required for Efficacy
J Med Chem 64: 5470-5484 (2021)
Lilly Research Laboratories
Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities.
J Med Chem 64: 6241-6261 (2021)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
J Med Chem 64: 4567-4587 (2021)
Heidelberg University
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
J Med Chem 64: 5067-5081 (2021)
Fudan University
An affinity prediction approach for the ligand of E3 ligase Cbl-b and an insight into substrate binding pattern.
Bioorg Med Chem 38: (2021)
China Pharmaceutical University
An insight into the medicinal attributes of berberine derivatives: A review.
Bioorg Med Chem 38: (2021)
Isf College Of Pharmacy
Identification of 2,2-Dimethylbutanoic Acid (HST5040), a Clinical Development Candidate for the Treatment of Propionic Acidemia and Methylmalonic Acidemia.
J Med Chem 64: 5037-5048 (2021)
Hemoshear Therapeutics
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at ?-Containing ?-Aminobutyric Acid Type A Receptors.
J Med Chem 64: 4730-4743 (2021)
University Of Copenhagen
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.
Eur J Med Chem 219: (2021)
University Of Chinese Academy Of Science
Further lead optimization on Bax activators: Design, synthesis and pharmacological evaluation of 2-fluoro-fluorene derivatives for the treatment of breast cancer.
Eur J Med Chem 219: (2021)
University Of Texas Medical Branch (Utmb)
Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
Eur J Med Chem 219: (2021)
Taipei Medical University
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.
Eur J Med Chem 219: (2021)
Guangzhou Medical University
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-
J Med Chem 64: 5404-5428 (2021)
University Of Turin
Bispecific Estrogen Receptor ? Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
J Med Chem 64: 5049-5066 (2021)
X-Chem
Synthesis of the Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor NB-360.
J Med Chem 64: 4677-4696 (2021)
TBA
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Bioorg Med Chem Lett 42: (2021)
Cracow University Of Technology
Design and identification of a new farnesoid X receptor (FXR) partial agonist by computational structure-activity relationship analysis: Ligand-induced H8 helix fluctuation in the ligand-binding domain of FXR may lead to partial agonism.
Bioorg Med Chem Lett 41: (2021)
Computer-Aided Molecular Modeling Research Center
Design, synthesis and in-vitro evaluation of fluorinated triazoles as multi-target directed ligands for Alzheimer disease.
Bioorg Med Chem Lett 42: (2021)
National Institute Of Pharmaceutical Education And Research (Niper) Ahmedabad
Synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenylpyrimidine derivatives with 4-amino or 4-hydroxy as a pharmacophore element binding with xanthine oxidase active site.
Bioorg Med Chem 38: (2021)
Shenyang Pharmaceutical University
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and ?-aminobutyric acid transporters.
Eur J Med Chem 218: (2021)
Jagiellonian University Medical College
Discovery of effective phosphodiesterase 2 inhibitors with antioxidant activities for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 41: (2021)
Sun Yat-Sen University
Prodrugs of a 1'-CN-4-Aza-7,9-dideazaadenosine
J Med Chem 64: 5001-5017 (2021)
Gilead Sciences
Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.
J Med Chem 64: 4762-4786 (2021)
Southern Research
Discovery of 5-(3-Chlorophenylamino)benzo[
J Med Chem 64: 5082-5098 (2021)
Southeast University
Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.
Eur J Med Chem 218: (2021)
Cha University
Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
Eur J Med Chem 218: (2021)
Institute Of Physiologically Active Compounds Russian Academy Of Sciences
Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
Eur J Med Chem 218: (2021)
Zhengzhou University
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors.
Bioorg Med Chem 38: (2021)
Nanjing Normal University
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
Bioorg Med Chem Lett 41: (2021)
National Institute Of Diabetes And Digestive And Kidney Diseases
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
J Med Chem 64: 4810-4840 (2021)
University Of Illinois At Chicago
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous
J Med Chem 64: 4430-4449 (2021)
Agios Pharmaceuticals
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.
J Med Chem 64: 4972-4990 (2021)
Alma Mater Studiorum - University Of Bologna
Tricyclic Triazoles as ?
J Med Chem 64: 5157-5170 (2021)
Esteve Pharmaceuticals
Discovery of new pyrimidopyrrolizine/indolizine-based derivatives as P-glycoprotein inhibitors: Design, synthesis, cytotoxicity, and MDR reversal activities.
Eur J Med Chem 218: (2021)
Umm Al-Qura University
Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation.
Eur J Med Chem 218: (2021)
University Of South Australia
Discovery and Optimization of 2
J Med Chem 64: 4913-4946 (2021)
National Center For Advancing Translational Sciences
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
J Med Chem 64: 4891-4902 (2021)
Lundbeck Research Usa
Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them.
J Med Chem 64: 4532-4552 (2021)
Lomonosov Moscow State University
Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists.
J Med Chem 64: 4697-4708 (2021)
Indiana University
Structure-Based Design of Selective LONP1 Inhibitors for Probing
J Med Chem 64: 4857-4869 (2021)
Genomics Institute Of The Novartis Research Foundation
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds.
J Med Chem 64: 4623-4661 (2021)
University Of Copenhagen
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
Eur J Med Chem 218: (2021)
China Pharmaceutical University
Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).
Bioorg Med Chem Lett 42: (2021)
Bristol-Myers Squibb
Discovery of novel Staphylococcus aureus penicillin binding protein 2a inhibitors by multistep virtual screening and biological evaluation.
Bioorg Med Chem Lett 41: (2021)
The First Affiliated Hospital Of Anhui Medical University
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.
Bioorg Med Chem 37: (2021)
University Of Wollongong
Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
Eur J Med Chem 218: (2021)
Shanghai Institute Of Pharmaceutical Industry
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.
Bioorg Med Chem Lett 41: (2021)
Sanford Burnham Prebys Medical Discovery Institute
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
J Med Chem 64: 4709-4729 (2021)
Merck
Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl-1.
J Med Chem 64: 4903-4912 (2021)
University Of California Riverside
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3K? Immunomodulators.
J Med Chem 64: 5137-5156 (2021)
Merck
Discovery of a Potent and Selective FLT3 Inhibitor (
J Med Chem 64: 4870-4890 (2021)
Nanjing University Of Chinese Medicine
Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration.
Eur J Med Chem 218: (2021)
Eberhard Karls Universit£T
Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.
J Med Chem 64: 5123-5136 (2021)
Goethe-University Frankfurt
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
J Med Chem 64: 4462-4477 (2021)
German University In Cairo
Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.
J Med Chem 64: 4588-4611 (2021)
China Pharmaceutical University
Structure-Activity Relationship of Heterocyclic P2Y
J Med Chem 64: 5099-5122 (2021)
National Institute Of Diabetes And Digestive And Kidney Diseases
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
Eur J Med Chem 218: (2021)
China Pharmaceutical University
Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors.
Eur J Med Chem 218: (2021)
Cairo University
Selective Discovery of GPCR Ligands within DNA-Encoded Chemical Libraries Derived from Natural Products: A Case Study on Antagonists of Angiotensin II Type I Receptor.
J Med Chem 64: 4196-4205 (2021)
Northwest University
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
J Med Chem 64: 3976-3996 (2021)
Peking University
Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.
J Med Chem 64: 5018-5036 (2021)
Charles River
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.
J Med Chem 64: 4289-4311 (2021)
University College London
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.
Eur J Med Chem 218: (2021)
Chinese Academy Of Sciences
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3
J Med Chem 64: 3940-3955 (2021)
Genentech
Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.
Bioorg Med Chem Lett 41: (2021)
Zhengzhou University
Structure-activity relationship studies of 3-substituted pyrazoles as novel allosteric inhibitors of MALT1 protease.
Bioorg Med Chem Lett 41: (2021)
Toray Industries
Discovery of N-amido-phenylsulfonamide derivatives as novel microsomal prostaglandin E
Bioorg Med Chem Lett 41: (2021)
Kyung Hee University
Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide.
Eur J Med Chem 218: (2021)
The First Affiliated Hospital Of Wenzhou Medical University
Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms.
Eur J Med Chem 218: (2021)
Saint Petersburg State University
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.
Bioorg Med Chem 37: (2021)
Wayne State University School Of Medicine
Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities.
Eur J Med Chem 218: (2021)
Kafrelsheikh University
FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.
Bioorg Med Chem Lett 41: (2021)
University Of Siena
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.
Bioorg Med Chem Lett 41: (2021)
Misr International University
Optimization of ether and aniline based inhibitors of lactate dehydrogenase.
Bioorg Med Chem Lett 41: (2021)
Vanderbilt University
Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold.
Eur J Med Chem 217: (2021)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.
J Med Chem 64: 4130-4149 (2021)
Sungkyunkwan University
Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects
J Med Chem 64: 3794-3812 (2021)
Julius Maximilian University Of W£Rzburg
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface.
J Med Chem 64: 3720-3746 (2021)
Goethe-University Frankfurt
Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening.
Bioorg Med Chem Lett 41: (2021)
Nanchang University
Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.
Bioorg Med Chem Lett 41: (2021)
Virginia Commonwealth University
The dual inhibition against the activity and expression of tyrosine phosphatase PRL-3 from a rhodanine derivative.
Bioorg Med Chem Lett 41: (2021)
Shanxi University
Synthesis, biological evaluation, and correlation of cytotoxicity versus redox potential of 1,4-naphthoquinone derivatives.
Bioorg Med Chem Lett 41: (2021)
National Research Institute Of Chinese Medicine
Rationally designed TNF-? inhibitors: Identification of promising cytotoxic agents.
Bioorg Med Chem Lett 41: (2021)
Guru Nanak Dev University
Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies.
Eur J Med Chem 217: (2021)
Shandong First Medical University & Shandong Academy Of Medical Sciences
Balancing potency and basicity by incorporating fluoropyridine moieties: Discovery of a 1-amino-3,4-dihydro-2,6-naphthyridine BACE1 inhibitor that affords robust and sustained central A? reduction.
Eur J Med Chem 216: (2021)
Shionogi Pharmaceutical Research Center
Designed ?-Hairpins Inhibit LDH5 Oligomerization and Enzymatic Activity.
J Med Chem 64: 3767-3779 (2021)
Queensland University Of Technology
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A
J Med Chem 64: 3827-3842 (2021)
Leiden University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
J Med Chem 64: 3508-3545 (2021)
Niddk
Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa).
J Med Chem 64: 3897-3910 (2021)
Institut De Recherches Servier
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists.
J Med Chem 64: 3870-3884 (2021)
The Scripps Research Institute
Allosteric Modulation: Dynamics is Double-"E"dged.
J Med Chem 64: 3694-3696 (2021)
Chinese Academy Of Sciences
Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines.
J Med Chem 64: 4150-4162 (2021)
The University Of Melbourne
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.
Bioorg Med Chem 37: (2021)
Cancer Hospital Of China Medical University
Development of phenyltriazole thiol-based derivatives as highly potent inhibitors of DCN1-UBC12 interaction.
Eur J Med Chem 217: (2021)
Zhengzhou University
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.
Eur J Med Chem 217: (2021)
University Of Texas Medical Branch
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
J Med Chem 64: 3911-3939 (2021)
Merck
Structure-Based Identification of Potent Lysine-Specific Demethylase 1 Inhibitor Peptides and Temporary Cyclization to Enhance Proteolytic Stability and Cell Growth-Inhibitory Activity.
J Med Chem 64: 3707-3719 (2021)
Nagoya City University
Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and ?
Bioorg Med Chem Lett 41: (2021)
Chiesi Farmaceutici
An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors.
Eur J Med Chem 217: (2021)
Shandong University
Using porphyrins as albumin-binding molecules to enhance antitumor efficacies and reduce systemic toxicities of antimicrobial peptides.
Eur J Med Chem 217: (2021)
Fuzhou University
Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib.
Eur J Med Chem 217: (2021)
Shanghaitech University
Structure-Activity Relationship Study of Dexrazoxane Analogues Reveals ICRF-193 as the Most Potent Bisdioxopiperazine against Anthracycline Toxicity to Cardiomyocytes Due to Its Strong Topoisomerase II? Interactions.
J Med Chem 64: 3997-4019 (2021)
Charles University
Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
J Med Chem 64: 3843-3869 (2021)
Genentech
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
J Med Chem 64: 4020-4033 (2021)
China Pharmaceutical University
Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
Eur J Med Chem 217: (2021)
Taipei Medical University
Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
Eur J Med Chem 217: (2021)
Second Military Medical University
Synthesis, biological evaluation, and docking studies of novel pyrrolo[2,3-b]pyridine derivatives as both ectonucleotide pyrophosphatase/phosphodiesterase inhibitors and antiproliferative agents.
Eur J Med Chem 217: (2021)
Comsats University Islamabad
Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides.
Eur J Med Chem 217: (2021)
Ataturk University
Discovery of antiproliferative and anti-FAK inhibitory activity of 1,2,4-triazole derivatives containing acetamido carboxylic acid skeleton.
Bioorg Med Chem Lett 40: (2021)
Deraya University
Discovery of 3-aryl substituted benzoxaboroles as broad-spectrum inhibitors of serine- and metallo-?-lactamases.
Bioorg Med Chem Lett 41: (2021)
Sichuan University
Development of new disulfiram analogues as ALDH1a1-selective inhibitors.
Bioorg Med Chem Lett 40: (2021)
Umm Al-Qura University
Discovery of 5-(N-hydroxycarbamimidoyl) benzofuran derivatives as novel indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
Bioorg Med Chem Lett 40: (2021)
Seoul National University
Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.
Eur J Med Chem 217: (2021)
Pla Strategic Support Force Medical Center
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.
Eur J Med Chem 217: (2021)
China Pharmaceutical University
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
ACS Med Chem Lett 12: 494-501 (2021)
Bristol Myers Squibb Research And Development
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1.
ACS Med Chem Lett 12: 485-493 (2021)
Purdue University
Identification of Potent Reverse Indazole Inhibitors for HPK1.
ACS Med Chem Lett 12: 459-466 (2021)
Merck
Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes.
ACS Med Chem Lett 12: 451-458 (2021)
Janssen Research & Development
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.
ACS Med Chem Lett 12: 420-425 (2021)
Hiroshima International University
Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.
ACS Med Chem Lett 12: 397-403 (2021)
Chinese Academy Of Sciences
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease.
ACS Med Chem Lett 12: 380-388 (2021)
Charles River Discovery
Biological Evaluation of 5'-(
ACS Med Chem Lett 12: 373-379 (2021)
National Institute Of Diabetes And Digestive And Kidney Diseases
Design and Structure-Activity Relationship of a Potent Furin Inhibitor Derived from Influenza Hemagglutinin.
ACS Med Chem Lett 12: 365-372 (2021)
University Of Gda?Sk
Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
ACS Med Chem Lett 12: 351-355 (2021)
Biogen
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.
ACS Med Chem Lett 12: 337-342 (2021)
Merck
Myeloid Cell Leukemia-1 Inhibitors as Emerging Cancer Treatment.
ACS Med Chem Lett 12: 334-336 (2021)
Therachem Research Medilab
Targeting Stimulator of Interferon Genes (STING) for the Potential Treatment of Cancer and Infectious Diseases.
ACS Med Chem Lett 12: 328-330 (2021)
Usona Institute
Tumor-Targeted Bivalent Protein Degradation for Application in Cancer Therapy.
ACS Med Chem Lett 12: 326-327 (2021)
Usona Institute
Novel Bicyclic Heterocycles as FGFR Inhibitors for Treating Cancer.
ACS Med Chem Lett 12: 320-321 (2021)
Smith, Gambrell & Russell
Novel Benzimidazole Derivatives as Transient Receptor Potential Channel 6 (TRPC6) Inhibitors.
ACS Med Chem Lett 12: 314-315 (2021)
Smith, Gambrell & Russell
Novel Oxazine Monoacylglycerol Lipase (MAGL) Inhibitors.
ACS Med Chem Lett 12: 312-313 (2021)
Smith, Gambrell & Russell
1-Pyrazolyl-5,6-Disubstituted Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.
ACS Med Chem Lett 12: 310-311 (2021)
Smith, Gambrell & Russell
Withanolides from dietary tomatillo suppress HT1080 cancer cell growth by targeting mutant IDH1.
Bioorg Med Chem 36: (2021)
Shenyang Pharmaceutical University
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
J Med Chem 64: 4239-4256 (2021)
Shandong University
Structure-Activity Relationship Studies on Oxazolo[3,4-
J Med Chem 64: 4089-4108 (2021)
University Of Ferrara
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
J Med Chem 64: 3956-3975 (2021)
Chinese Academy Of Sciences
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.
ACS Med Chem Lett 12: 443-450 (2021)
Bristol Myers Squibb
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.
ACS Med Chem Lett 12: 426-432 (2021)
Philipps University
Ring closure strategy leads to potent RIPK3 inhibitors.
Eur J Med Chem 217: (2021)
Soochow University
Recent advances in development of hetero-bivalent kinase inhibitors.
Eur J Med Chem 216: (2021)
Cha University
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.
J Med Chem 64: 3677-3693 (2021)
Athenex
Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion.
J Med Chem 64: 3658-3676 (2021)
Reviral
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
Eur J Med Chem 216: (2021)
Zhejiang University
One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
Eur J Med Chem 216: (2021)
The Affiliated Hospital Of Qingdao University
Design, synthesis, and biological evaluation of nitroisoxazole-containing spiro[pyrrolidin-oxindole] derivatives as novel glutathione peroxidase 4/mouse double minute 2 dual inhibitors that inhibit breast adenocarcinoma cell proliferation.
Eur J Med Chem 217: (2021)
Chengdu University Of Traditional Chinese Medicine
Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention.
J Med Chem 64: 3813-3826 (2021)
University Of East Anglia
C@PA: Computer-Aided Pattern Analysis to Predict Multitarget ABC Transporter Inhibitors.
J Med Chem 64: 3350-3366 (2021)
University Of Bonn
Alkyne-Bridged ?-Conotoxin Vc1.1 Potently Reverses Mechanical Allodynia in Neuropathic Pain Models.
J Med Chem 64: 3222-3233 (2021)
Monash University
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A
J Med Chem 64: 6670-6695 (2021)
Monash University
Developing novel classes of protein kinase CK1? inhibitors by fusing [1,2,4]triazole with different bicyclic heteroaromatic systems.
Eur J Med Chem 216: (2021)
Universit£
Structural insights of oxindole based kinase inhibitors as anticancer agents: Recent advances.
Eur J Med Chem 216: (2021)
National Institute Of Pharmaceutical Education And Research (Niper)
Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations.
J Med Chem 64: 3100-3114 (2021)
Sookmyung Women'S University
Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor.
J Med Chem 64: 3439-3448 (2021)
Lilly Research Laboratories
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
J Med Chem 64: 2937-2952 (2021)
Galapagos
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
J Med Chem 64: 2878-2900 (2021)
China Pharmaceutical University
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective ?-Secretase (BACE1) Inhibitors over BACE2.
J Med Chem 64: 3075-3085 (2021)
Shionogi Pharmaceutical Research Center
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.
J Med Chem 64: 6569-6580 (2021)
Boehringer Ingelheim Rcv
Discovery of Selective Pituitary Adenylate Cyclase 1 Receptor (PAC1R) Antagonist Peptides Potent in a Maxadilan/PACAP38-Induced Increase in Blood Flow Pharmacodynamic Model.
J Med Chem 64: 3427-3438 (2021)
Amgen
Design, Synthesis, and Evaluation of Small Molecule G?q/11 Protein Inhibitors for the Treatment of Uveal Melanoma.
J Med Chem 64: 3131-3152 (2021)
Sun Yat-Sen University
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.
Eur J Med Chem 216: (2021)
Nirma University
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.
Eur J Med Chem 216: (2021)
Institute For Organic Syntheses (Vuos)
IDO1 and TDO inhibitory evaluation of analogues of the marine pyrroloiminoquinone alkaloids: Wakayin and Tsitsikammamines.
Bioorg Med Chem Lett 40: (2021)
Universit£
Addition of hydrophobic side chains improve the apoptosis inducibility of the human glyoxalase I inhibitor, TLSC702.
Bioorg Med Chem Lett 40: (2021)
Tokyo University Of Science
Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting.
J Med Chem 64: 3204-3221 (2021)
University Of Modena And Reggio Emilia
Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
Eur J Med Chem 216: (2021)
Universities Of Shandong
The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition.
Bioorg Med Chem Lett 40: (2021)
Beijing University Of Technology
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
Bioorg Med Chem Lett 40: (2021)
Huazhong University Of Science And Technology
A novel class of selective non-nucleoside inhibitors of human DNA methyltransferase 3A.
Bioorg Med Chem Lett 40: (2021)
University Of California
Cyclic Analogues of the Chemerin C-Terminus Mimic a Loop Conformation Essential for Activating the Chemokine-like Receptor 1.
J Med Chem 64: 3048-3058 (2021)
Leipzig University
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.
J Med Chem 64: 3234-3248 (2021)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice.
J Med Chem 64: 3006-3025 (2021)
Rti International
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.
Bioorg Med Chem Lett 40: (2021)
Sumitomo Dainippon Pharma.
Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties.
Eur J Med Chem 216: (2021)
Chung-Ang University
Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.
Eur J Med Chem 216: (2021)
Fudan University
One pot synthesis, in silico study and evaluation of some novel flavonoids as potent topoisomerase II inhibitors.
Bioorg Med Chem Lett 40: (2021)
Dr. Babasaheb Ambedkar Marathwada University
Discovery and characterization of a novel glucose-6-phosphate dehydrogenase (G6PD) inhibitor via high-throughput screening.
Bioorg Med Chem Lett 40: (2021)
Nanjing University Of Chinese Medicine
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
J Med Chem 64: 3086-3099 (2021)
Bristol Myers Squibb
Conformational Constraint between Aromatic Residue Side Chains in the "Message" Sequence of the Peptide Arodyn Using Ring Closing Metathesis Results in a Potent and Selective Kappa Opioid Receptor Antagonist.
J Med Chem 64: 3153-3164 (2021)
The University Of Kansas
Current status in the discovery of dual BET/HDAC inhibitors.
Bioorg Med Chem Lett 38: (2021)
The First Affiliated Hospital Of Zhengzhou University
Design, synthesis, biological evaluation and structure-activity relationship study of quinazolin-4(3H)-one derivatives as novel USP7 inhibitors.
Eur J Med Chem 216: (2021)
Zhengzhou University
Novel monocyclic amide-linked phenol derivatives without mitochondrial toxicity have potent uric acid-lowering activity.
Bioorg Med Chem Lett 40: (2021)
Fuji Yakuhin
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
Bioorg Med Chem Lett 39: (2021)
Astrazeneca
Heparan Sulfate Mimetics Differentially Affect Homologous Chemokines and Attenuate Cancer Development.
J Med Chem 64: 3367-3380 (2021)
Indian Institute Of Science Education And Research
Dihydro-?-agarofuran-Type Sesquiterpenoids from the Seeds of
J Nat Prod 84: 588-600 (2021)
Chinese Academy Of Sciences
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.
J Med Chem 64: 3165-3184 (2021)
Astrazeneca
Discovery of a Potent and Orally Bioavailable Melatonin Receptor Agonist.
J Med Chem 64: 3059-3074 (2021)
Takeda Pharmaceutical
Discovery of deoxyceramide analogs as highly selective ACER3 inhibitors in live cells.
Eur J Med Chem 216: (2021)
Institute For Advanced Chemistry Of Catalonia (Iqac-Csic)
Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38? MAP inhibitors.
Eur J Med Chem 216: (2021)
Yanbian University
Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
Bioorg Med Chem 35: (2021)
University Of S£O Paulo
Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.
Bioorg Med Chem 36: (2021)
Southeast University
A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.
Eur J Med Chem 216: (2021)
University Of Louisiana At Monroe
Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors.
Eur J Med Chem 216: (2021)
Kafrelsheikh University
Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.
Eur J Med Chem 216: (2021)
Nanyang Normal University
Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y
Eur J Med Chem 216: (2021)
China Pharmaceutical University
Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.
J Med Chem 64: 3299-3319 (2021)
University Of Sheffield
Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors.
J Med Chem 64: 3320-3349 (2021)
Technical University Darmstadt
3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum.
J Med Chem 64: 3035-3047 (2021)
Heinrich Heine University D£Sseldorf
A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease.
Eur J Med Chem 215: (2021)
Indian Institute Of Technology (Banaras Hindu University)
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.
Bioorg Med Chem Lett 41: (2021)
Sichuan University
Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator.
Bioorg Med Chem Lett 40: (2021)
Cyclerion Therapeutics
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J Med Chem 64: 3249-3281 (2021)
Glaxosmithkline
Freshwater Fungi as a Source of Chemical Diversity: A Review.
J Nat Prod 84: 898-916 (2021)
Jordan University Of Science And Technology
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
J Med Chem 64: 3392-3426 (2021)
University Of Navarra
Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.
Eur J Med Chem 216: (2021)
University Of Arkansas For Medical Sciences
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
Bioorg Med Chem 35: (2021)
Duquesne University
Design, synthesis, and evaluation of a novel prodrug, a S-trityl-
Eur J Med Chem 215: (2021)
University Of Shizuoka
Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Bioorg Med Chem 35: (2021)
Guizhou Medical University
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors.
Eur J Med Chem 216: (2021)
Southeast University
Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors.
Bioorg Med Chem Lett 39: (2021)
National Institute Of Pharmaceutical Education And Research (Niper)
A new class of ?-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities.
Eur J Med Chem 215: (2021)
Tsinghua University
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.
Eur J Med Chem 215: (2021)
Masaryk University
Medulloblastoma drugs in development: Current leads, trials and drawbacks.
Eur J Med Chem 215: (2021)
University Of Connecticut
Oxa-adamantyl cannabinoids.
Bioorg Med Chem Lett 38: (2021)
University Of Hawaii At Manoa
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT
Bioorg Med Chem Lett 38: (2021)
Arena Pharmaceuticals
Structure based design and synthesis of novel Toll-like Receptor 2 (TLR 2) lipid antagonists.
Bioorg Med Chem Lett 40: (2021)
Neuropore Therapies
Exploring the Chemistry of Alkaloids from Malaysian
J Nat Prod 84: 1034-1043 (2021)
Universiti Sains Malaysia
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
J Med Chem 64: 2501-2520 (2021)
Millennium Pharmaceuticals, A Wholly Owned Subsidiary Of Takeda Pharmaceuticals
Structure-Activity Relationship Studies of Coumarin-like Diacid Derivatives as Human G Protein-Coupled Receptor-35 (hGPR35) Agonists and a Consequent New Design Principle.
J Med Chem 64: 2634-2647 (2021)
Chinese Academy Of Sciences
Fragment-like Chloroquinolineamines Activate the Orphan Nuclear Receptor Nurr1 and Elucidate Activation Mechanisms.
J Med Chem 64: 2659-2668 (2021)
Goethe University
Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.
J Med Chem 64: 2669-2677 (2021)
Taiho Pharmaceutical
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
J Nat Prod 84: 1104-1112 (2021)
University Of Florida
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPAR? Modulator.
J Med Chem 64: 2815-2828 (2021)
Goethe University
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.
Eur J Med Chem 214: (2021)
Wenzhou Medical University
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.
Eur J Med Chem 215: (2021)
Shanghaitech University
Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
Eur J Med Chem 215: (2021)
Fourth Military Medical University
Discovery of a novel potent cytochrome P450 CYP4Z1 inhibitor.
Eur J Med Chem 215: (2021)
Freie Universit£T Berlin
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes.
Bioorg Med Chem 35: (2021)
M. S. University Of Baroda
3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation.
Bioorg Med Chem Lett 37: (2021)
National Institute Of Pharmaceutical Education And Research (Niper)
Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding.
Bioorg Med Chem Lett 38: (2021)
University Of Auckland
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Bioorg Med Chem Lett 38: (2021)
Roche Innovation Center Shanghai
Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva.
Bioorg Med Chem Lett 38: (2021)
Riken Center For Sustainable Resource Science
Design, synthesis and bioactivity evaluation of novel pyrazole linked phenylthiazole derivatives in context of antibacterial activity.
Bioorg Med Chem Lett 39: (2021)
Griffith University
Pyridones in drug discovery: Recent advances.
Bioorg Med Chem Lett 38: (2021)
Astrazeneca
Design and synthesis of a monocyclic derivative as a selective ACC1 inhibitor by chemical modification of biphenyl ACC1/2 dual inhibitors.
Bioorg Med Chem 35: (2021)
Takeda Pharmaceutical
Synthesis and evaluation of cyclopentane-based muraymycin analogs targeting MraY.
Eur J Med Chem 215: (2021)
Duke University
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.
J Med Chem 64: 2829-2848 (2021)
Sichuan University
Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
ACS Med Chem Lett 12: 302-308 (2021)
Astrazeneca
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
ACS Med Chem Lett 12: 288-294 (2021)
Bristol Myers Squibb Research And Development
A New FXR Ligand Chemotype with Agonist/Antagonist Switch.
ACS Med Chem Lett 12: 267-274 (2021)
Goethe-University Frankfurt
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
ACS Med Chem Lett 12: 249-255 (2021)
Yale University
Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication.
ACS Med Chem Lett 12: 242-248 (2021)
Korea Research Institute Of Chemical Technology
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
ACS Med Chem Lett 12: 236-241 (2021)
National Institute Of Health Sciences
Virtual Screening Approach to Identifying a Novel and Tractable Series of
ACS Med Chem Lett 12: 217-227 (2021)
Antabio
Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors.
ACS Med Chem Lett 12: 211-216 (2021)
Kogakuin University
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides.
ACS Med Chem Lett 12: 202-210 (2021)
National Institutes Of Health (Nih) National Center Of Excellence For Computational Drug Abuse Research
Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors.
ACS Med Chem Lett 12: 195-201 (2021)
Shanghai Hengrui Pharmaceutical
Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.
ACS Med Chem Lett 12: 182-184 (2021)
Therachem Research Medilab
Methionine Adenosyltransferase Inhibitors for the Treatment of Cancer.
ACS Med Chem Lett 12: 180-181 (2021)
Usona Institute
Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer's Disease.
ACS Med Chem Lett 12: 178-179 (2021)
Usona Institute
Novel Galectin-3 Inhibitors for Treating Fibrosis.
ACS Med Chem Lett 12: 174-175 (2021)
Smith, Gambrell & Russell
Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).
ACS Med Chem Lett 12: 170-171 (2021)
Smith, Gambrell & Russell
SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse model
Science (2021)
Sichuan University
Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity.
Eur J Med Chem 215: (2021)
University Of Siena
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF
Eur J Med Chem 215: (2021)
Korea Institute Of Science & Technology (Kist School)
Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling.
Eur J Med Chem 215: (2021)
University Of Houston
Synthesis of Yakuchinone B-Inspired Inhibitors against Islet Amyloid Polypeptide Aggregation.
J Nat Prod 84: 1096-1103 (2021)
Taipei Medical University
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.
J Med Chem 64: 2608-2621 (2021)
Leiden Academic Centre For Drug Research
C-2-Linked Dimeric Strychnine Analogues as Bivalent Ligands Targeting Glycine Receptors.
J Nat Prod 84: 382-394 (2021)
The German University In Cairo
Synthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease.
J Med Chem 64: 2777-2800 (2021)
Baylor College Of Medicine
Discovery of 3-(4-(2-((1
J Med Chem 64: 1966-1988 (2021)
West China Hospital Of Sichuan University
Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A
J Med Chem 64: 1889-1903 (2021)
TBA
CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia.
J Med Chem 64: 1835-1843 (2021)
Bristol Myers Squibb
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.
J Med Chem 64: 3697-3706 (2021)
Icahn School Of Medicine At Mount Sinai
Tricyclic-Carbocyclic ROR?t Inverse Agonists-Discovery of BMS-986313.
J Med Chem 64: 2714-2724 (2021)
Bristol Myers Squibb
Bicyclic Diazepinones as Dual Ligands of the ?2?-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
J Med Chem 64: 2167-2185 (2021)
Esteve Pharmaceuticals
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based ?-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
J Med Chem 64: 1873-1888 (2021)
Janssen Research & Development
Discovery and structural optimization of 3-O-?-chacotriosyl oleanane-type triterpenoids as potent entry inhibitors of SARS-CoV-2 virus infections.
Eur J Med Chem 215: (2021)
South China Agricultural University
Antitubercular properties of thiazolidin-4-ones - A review.
Eur J Med Chem 215: (2021)
Medical University Of Lublin
CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
Eur J Med Chem 215: (2021)
Taipei Medical University
Multifunctional agents based on benzoxazolone as promising therapeutic drugs for diabetic nephropathy.
Eur J Med Chem 215: (2021)
Beijing Institute Of Technology
Discovery of Novel Pyrrolo[2,3-
J Med Chem 65: 1243-1264 (2022)
Chinese Academy Of Sciences
Discovery of new phenyl sulfonyl-pyrimidine carboxylate derivatives as the potential multi-target drugs with effective anti-Alzheimer's action: Design, synthesis, crystal structure and in-vitro biological evaluation.
Eur J Med Chem 215: (2021)
Jamia Millia Islamia
Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands.
Eur J Med Chem 215: (2021)
Palack£
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.
Eur J Med Chem 214: (2021)
Florida A&M University
Targeting SHP2 as a therapeutic strategy for inflammatory diseases.
Eur J Med Chem 214: (2021)
Shenyang Pharmaceutical University
Annual review of LSD1/KDM1A inhibitors in 2020.
Eur J Med Chem 214: (2021)
Beijing University Of Chinese Medicine
Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects.
Eur J Med Chem 214: (2021)
Shenyang Pharmaceutical University
Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II.
Eur J Med Chem 214: (2021)
University Of Florence
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.
Eur J Med Chem 214: (2021)
University Of Nottingham
Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor.
Bioorg Med Chem 34: (2021)
Toho University
Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype.
J Med Chem 64: 2691-2704 (2021)
University Of Toronto Mississauga
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite
J Med Chem 64: 2291-2309 (2021)
University Of Cape Town
Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M
Eur J Med Chem 213: (2021)
University Of Regensburg
Discovery of a novel 53BP1 inhibitor through AlphaScreen-based high-throughput screening.
Bioorg Med Chem 34: (2021)
Yantai University
Synthesis and preliminary anticancer evaluation of new triazole bisphosphonate-based isoprenoid biosynthesis inhibitors.
Eur J Med Chem 214: (2021)
Universit£
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
Eur J Med Chem 214: (2021)
University Of South Australia
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.
Bioorg Med Chem Lett 37: (2021)
Sungkyunkwan University
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
J Med Chem 64: 1844-1855 (2021)
Chinese Academy Of Sciences
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
J Med Chem 64: 2228-2241 (2021)
Moffitt Cancer Center
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
J Med Chem 64: 2186-2204 (2021)
The University Of Queensland
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.
Eur J Med Chem 214: (2021)
Shandong University
Structural optimization towards promising ?-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation.
Eur J Med Chem 214: (2021)
Jiaxing University
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
J Med Chem 64: 2272-2290 (2021)
Universidad Aut£Noma De Madrid
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of
J Nat Prod 84: 436-443 (2021)
Chinese Academy Of Sciences
Azole-Based Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors.
J Med Chem 64: 2205-2227 (2021)
Sib Swiss Institute Of Bioinformatics
Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant.
Bioorg Med Chem 34: (2021)
Nagasaki University
Discovery and optimization of a novel CNS penetrant series of mGlu
Bioorg Med Chem Lett 37: (2021)
Vanderbilt University
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
J Med Chem 64: 2139-2150 (2021)
Sanofi R&D
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative.
J Med Chem 64: 1856-1872 (2021)
Eicosis Human Health
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.
Eur J Med Chem 214: (2021)
University Of Minnesota
Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity.
Eur J Med Chem 214: (2021)
Chongqing University
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
Bioorg Med Chem 33: (2021)
University Of Tennessee Health Science Center
Chemical validation of a druggable site on Hsp27/HSPB1 using in silico solvent mapping and biophysical methods.
Bioorg Med Chem 34: (2021)
University Of California At San Francisco
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model.
Bioorg Med Chem 34: (2021)
Kyorin Pharmaceutical
Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach.
Bioorg Med Chem 34: (2021)
Takeda Pharmaceutical
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H
Eur J Med Chem 214: (2021)
University Of Regensburg
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
Eur J Med Chem 214: (2021)
University Of Cologne
Amyloid-? and tau aggregation dual-inhibitors: A synthetic and structure-activity relationship focused review.
Eur J Med Chem 214: (2021)
University Of Aveiro
Synthesis and evaluation of novel cyclopentane urea FPR2 agonists and their potential application in the treatment of cardiovascular inflammation.
Eur J Med Chem 214: (2021)
Queen Mary University Of London
Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
Eur J Med Chem 214: (2021)
Beni-Suef University
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.
J Med Chem 64: 2010-2023 (2021)
Sun Yat-Sen University
Discovery of Novel
J Med Chem 64: 2254-2271 (2021)
East China University Of Science And Technology
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
Eur J Med Chem 214: (2021)
Zhengzhou University
Discovery of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor: Scaffold hopping approach.
Eur J Med Chem 214: (2021)
Gedeon Richter
HIV latency reversal agents: A potential path for functional cure?
Eur J Med Chem 213: (2021)
S£O Paulo State University (Unesp)
Dioxotriazine derivatives as a new class of P2X
Bioorg Med Chem Lett 37: (2021)
Shionogi
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
J Med Chem 65: 893-921 (2022)
Csir-Indian Institute Of Integrative Medicine
Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic.
J Med Chem 64: 2110-2124 (2021)
Universit£
Chemical Highlights Supporting the Role of Lipid A in Efficient Biological Adaptation of Gram-Negative Bacteria to External Stresses.
J Med Chem 64: 1816-1834 (2021)
Aix Marseille Universit£
Metalloaminopeptidases of the Protozoan Parasite
J Med Chem 64: 1763-1785 (2021)
University Of Leeds
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
J Med Chem 64: 1989-2009 (2021)
Hacettepe University
Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug.
J Med Chem 64: 1725-1732 (2021)
TBA
Discovery of 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol Derivatives as Glutathione Transferase Inhibitors with Favorable Selectivity and Tolerated Toxicity.
J Med Chem 64: 1701-1712 (2021)
Southeast University
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.
Eur J Med Chem 213: (2021)
University Of Ljubljana
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
J Med Chem 64: 5345-5364 (2021)
Universit£
Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.
J Med Chem 64: 1685-1700 (2021)
Veterans Affairs Medical Center
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.
J Med Chem 64: 1362-1391 (2021)
Zhengzhou University
Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer.
J Med Chem 64: 1713-1724 (2021)
University Of Florida
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.
J Med Chem 64: 1584-1592 (2021)
University Of Toronto
Bisphosphonates, Old Friends of Bones and New Trends in Clinics.
J Med Chem 64: 1260-1282 (2021)
University Of Aveiro
Insights into non-peptide small-molecule inhibitors of the PD-1/PD-L1 interaction: Development and perspective.
Bioorg Med Chem 33: (2021)
Shenyang Pharmaceutical University
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.
Eur J Med Chem 213: (2021)
University Of South Australia
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
Eur J Med Chem 213: (2021)
Anhui Medical University
Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors.
Bioorg Med Chem Lett 36: (2021)
China Pharmaceutical University
Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91.
J Med Chem 64: 1626-1648 (2021)
University Of Michigan
A High-Affinity Peptide Ligand Targeting Syntenin Inhibits Glioblastoma.
J Med Chem 64: 1423-1434 (2021)
University Of Copenhagen
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3?.
J Med Chem 64: 1497-1509 (2021)
University Of Central Lancashire
Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase.
Eur J Med Chem 213: (2021)
Ku Leuven
Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70.
J Med Chem 64: 1733-1761 (2021)
St. Jude Children'S Research Hospital
Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors.
J Med Chem 64: 1481-1496 (2021)
Tokyo Medical And Dental University (Tmdu)
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
Eur J Med Chem 213: (2021)
Tsinghua University
Design, synthesis and biological evaluation of novel 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl)acetamide derivatives as potent VEGFR-2 inhibitors.
Eur J Med Chem 213: (2021)
Lanzhou University
Discovery of a novel family of FKBP12 "reshapers" and their use as calcium modulators in skeletal muscle under nitro-oxidative stress.
Eur J Med Chem 213: (2021)
Universidad Del Pa£S Vasco Upv/Ehu
4-Oxoquinolines and monoamine oxidase: When tautomerism matters.
Eur J Med Chem 213: (2021)
Universit£"Magna Gr£Cia" Di Catanzaro
Discovery of 6-Oxo-4-phenyl-hexanoic acid derivatives as ROR?t inverse agonists showing favorable ADME profile.
Bioorg Med Chem Lett 36: (2021)
Teijin Pharma
Bicyclic Ligand-Biased Agonists of S1P
J Med Chem 64: 1454-1480 (2021)
Bristol Myers Squibb Research & Early Development
Copper(I)-Catalyzed Nitrile-Addition/
J Med Chem 64: 1435-1453 (2021)
National Chiayi University
Secondary Metabolites from the Leather Coral-Derived Fungal Strain
J Nat Prod 84: 466-473 (2021)
University Of Hawai'I At Hilo
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
ACS Med Chem Lett 12: 162-167 (2021)
Astrazeneca
Discovery of PIPE-359, a Brain-Penetrant, Selective M
ACS Med Chem Lett 12: 155-161 (2021)
Pipeline Therapeutics
Discovery of a Series of Pyrazinone ROR? Antagonists and Identification of the Clinical Candidate BI 730357.
ACS Med Chem Lett 12: 143-154 (2021)
Boehringer Ingelheim Pharmaceuticals
Synthesis and Metabolism of BTN3A1 Ligands: Studies on Modifications of the Allylic Alcohol.
ACS Med Chem Lett 12: 136-142 (2021)
University Of Iowa
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.
ACS Med Chem Lett 12: 129-135 (2021)
Vertex Pharmaceuticals
Multiresidue Tetrapeptide Substitutions Yield a 140-fold Selective Melanocortin-3 over Melanocortin-4 Receptor Agonist.
ACS Med Chem Lett 12: 115-120 (2021)
University Of Minnesota
Solution Conformations Shed Light on PROTAC Cell Permeability.
ACS Med Chem Lett 12: 107-114 (2021)
Uppsala University
Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
ACS Med Chem Lett 12: 99-106 (2021)
Merck
Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
ACS Med Chem Lett 12: 93-98 (2021)
H3 Biomedicine
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.
ACS Med Chem Lett 12: 82-87 (2021)
Chinese Academy Of Sciences
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.
ACS Med Chem Lett 12: 74-81 (2021)
Max Planck Institute For Developmental Biology
Design and Synthesis of Fragment Derivatives with a Unique Inhibition Mechanism of the uPAR·uPA Interaction.
ACS Med Chem Lett 12: 60-66 (2021)
Indiana University School Of Medicine
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group.
ACS Med Chem Lett 12: 39-47 (2021)
Shenyang Pharmaceutical University
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.
ACS Med Chem Lett 12: 30-38 (2021)
Dana-Farber Cancer Institute
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.
ACS Med Chem Lett 12: 24-29 (2021)
Reaction Biology
Cyclin-Dependent Kinase Inhibitors in Cancer Therapeutics.
ACS Med Chem Lett 12: 11-12 (2021)
Usona Institute
Novel Pyrimidinones as SHP2 Antagonists for Treating Cancer.
ACS Med Chem Lett 12: 3-4 (2021)
Smith, Gambrell & Russell
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.
Bioorg Med Chem 33: (2021)
Astellas Pharma
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.
Eur J Med Chem 213: (2021)
China Pharmaceutical University
A theranostic probe of indoleamine 2,3-dioxygenase 1 (IDO1) for small molecule cancer immunotherapy.
Eur J Med Chem 213: (2021)
Second Military Medical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
J Med Chem 64: 1283-1345 (2021)
Hefei University Of Technology
Novel 1,3,4-thiadiazole compounds as potential MAO-A inhibitors - design, synthesis, biological evaluation and molecular modelling.
RSC Med Chem 11: 1063-1074 (2020)
Anadolu University
Fenretinide binding to the lysosomal protein saposin D alters ceramide solubilization and hydrolysis.
RSC Med Chem 11: 1048-1052 (2020)
Syracuse University
Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor.
RSC Med Chem 11: 1032-1040 (2020)
University Of Bern
Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation.
RSC Med Chem 11: 1023-1031 (2020)
University Of Bern
Recent developments of small molecule ?-secretase modulators for Alzheimer's disease.
RSC Med Chem 11: 1003-1022 (2020)
Memorial Sloan-Kettering Cancer Center
Histone lysine specific demethylase 1 inhibitors.
RSC Med Chem 11: 969-981 (2020)
Taipei Medical University
Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin ?V?3 and PAR2.
RSC Med Chem 11: 940-949 (2020)
Marquette University
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism
RSC Med Chem 11: 923-939 (2020)
Central University Of Punjab
G-Protein biased opioid agonists: 3-hydroxy-
RSC Med Chem 11: 896-904 (2020)
National Institute On Drug Abuse
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against
RSC Med Chem 11: 885-895 (2020)
University Of Washington
Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M
RSC Med Chem 11: 823-832 (2020)
University Of Regensburg
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.
RSC Med Chem 11: 707-731 (2020)
Newcastle University
Understanding the mechanism of action of pyrrolo[3,2-
RSC Med Chem 11: 665-675 (2020)
University Of Zurich
Online informatics resources to facilitate cancer target and chemical probe discovery.
RSC Med Chem 11: 611-624 (2020)
Emory University School Of Medicine
Computer-aided discovery of phenylpyrazole based amides as potent S6K1 inhibitors.
RSC Med Chem 11: 583-590 (2020)
Shanghai Institute Of Technology
Discovery, SAR study and ADME properties of methyl 4-amino-3-cyano-1-(2-benzyloxyphenyl)-1
RSC Med Chem 11: 577-582 (2020)
Universit£
Synthesis, evaluation and molecular modelling of piceatannol analogues as arginase inhibitors.
RSC Med Chem 11: 559-568 (2020)
Univ. Bourgogne Franche-Comt�
Discovery of a novel kinase hinge binder fragment by dynamic undocking.
RSC Med Chem 11: 552-558 (2020)
Universitat De Barcelona
Arylsulfonyl histamine derivatives as powerful and selective ?-glucosidase inhibitors.
RSC Med Chem 11: 518-527 (2020)
Universidad Nacional De Rosario
Reversing binding sensitivity to A147T translocator protein.
RSC Med Chem 11: 511-517 (2020)
The University Of Sydney
Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?
RSC Med Chem 11: 455-490 (2020)
University Of Cape Town
Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives.
RSC Med Chem 11: 378-386 (2020)
University Of Belgrade
Synthetic inhibitor leads of human tropomyosin receptor kinase A (
RSC Med Chem 11: 370-377 (2020)
Zoetis
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
RSC Med Chem 11: 307-316 (2020)
School Of Health Sciences/Graduate Program In Pharmaceutical Sciences
Argininamide-type neuropeptide Y Y
RSC Med Chem 11: 274-282 (2020)
University Of Regensburg
Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3).
RSC Med Chem 11: 268-273 (2020)
University Of Porto
Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP).
RSC Med Chem 11: 234-244 (2020)
Uppsala University
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
RSC Med Chem 11: 225-233 (2020)
China Pharmaceutical University
An epigrammatic status of the '
RSC Med Chem 11: 184-211 (2020)
Uttaranchal University
Identification of 6-amino-1
RSC Med Chem 11: 1168-1177 (2020)
University Of Dundee
Recent progress in the discovery of ghrelin
RSC Med Chem 11: 1136-1144 (2020)
National Institute On Alcohol Abuse And Alcoholism
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-
RSC Med Chem 11: 1112-1135 (2020)
University Of Edinburgh
Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.
RSC Med Chem 11: 125-131 (2020)
Virginia Commonwealth University
Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
Bioorg Med Chem 32: (2021)
Qom University Of Medical Sciences
A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cells.
Eur J Med Chem 213: (2021)
California Institute Of Technology
Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
Eur J Med Chem 213: (2021)
Jiangxi University Of Traditional Chinese Medicine
In silico drug repositioning on F508del-CFTR: A proof-of-concept study on the AIFA library.
Eur J Med Chem 213: (2021)
National Research Council (Itb-Cnr)
Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design.
J Med Chem 64: 1558-1569 (2021)
West China Hospital Of Sichuan University
How a Fragment Draws Attention to Selectivity Discriminating Features between the Related Proteases Trypsin and Thrombin.
J Med Chem 64: 1611-1625 (2021)
Philipps-Universit£T Marburg
Structure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists.
J Med Chem 64: 1649-1669 (2021)
Chinese Academy Of Sciences
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
J Med Chem 64: 909-924 (2021)
Janssen Research And Development
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments.
Bioorg Med Chem Lett 36: (2021)
China Pharmaceutical University
Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer.
J Med Chem 64: 925-937 (2021)
Zhengzhou University
Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation.
Eur J Med Chem 213: (2021)
Zhejiang University
Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.
Eur J Med Chem 212: (2021)
Rheinische Friedrich-Wilhelms-University Of Bonn
A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity.
Bioorg Med Chem Lett 36: (2021)
Daiichi Sankyo
Discovery of a PROTAC targeting ALK with in vivo activity.
Eur J Med Chem 212: (2021)
West China Hospital Of Sichuan University
Discovery of a true bivalent dopamine D
Eur J Med Chem 212: (2021)
Changzhou University
Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis.
J Med Chem 64: 1127-1138 (2021)
Syracuse University
Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.
Eur J Med Chem 212: (2021)
Virginia Tech
The subgroup of 2'-hydroxy-flavonoids: Molecular diversity, mechanism of action, and anticancer properties.
Bioorg Med Chem 32: (2021)
Oncowitan
Berberine Directly Targets the NEK7 Protein to Block the NEK7-NLRP3 Interaction and Exert Anti-inflammatory Activity.
J Med Chem 64: 768-781 (2021)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.
Bioorg Med Chem 32: (2021)
Henan University
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3?.
Bioorg Med Chem 32: (2021)
Charles University
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.
Bioorg Med Chem 32: (2021)
Maternal And Child Health Hospital Of Hubei Province
Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation.
Bioorg Med Chem 32: (2021)
State University Of Maring£
Structure-Activity Relationship and Biological Investigation of SR18292 (
J Med Chem 64: 980-990 (2021)
The Scripps Research Institute
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR
Eur J Med Chem 212: (2021)
Sun Yat-Sen University
Discovery and Biological Evaluation of
J Med Chem 64: 958-979 (2021)
Ewha Womans University
The Development of Hsp90?-Selective Inhibitors to Overcome Detriments Associated with
J Med Chem 64: 1545-1557 (2021)
The University Of Notre Dame
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
J Med Chem 64: 1170-1179 (2021)
Westf£Lische Wilhelms-Universit£T M£Nster
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPAR?) Partial Agonists:?Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities.
J Med Chem 64: 1018-1036 (2021)
Chongqing Medical University
Design of novel Xenopus GLP-1-based dual glucagon-like peptide 1 (GLP-1)/glucagon receptor agonists.
Eur J Med Chem 212: (2021)
Affiliated Tumor Hospital Of Guangxi Medical University
Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions.
Eur J Med Chem 212: (2021)
City University Of Hong Kong
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.
Eur J Med Chem 212: (2021)
Istanbul Medipol University
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38?/MAPK14 inhibitor.
Bioorg Med Chem 31: (2021)
University Of Science & Technology (Ust)
Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Bioorg Med Chem 31: (2021)
Chemveda Life Sciences India
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-?t (ROR?t) agonists.
Bioorg Med Chem Lett 35: (2021)
Bristol Myers Squibb
Peripheral Selective Oxadiazolylphenyl Alanine Derivatives as Tryptophan Hydroxylase 1 Inhibitors for Obesity and Fatty Liver Disease.
J Med Chem 64: 1037-1053 (2021)
Gwangju Institute Of Science And Technology
Discovery of a Novel and Brain-Penetrant
J Med Chem 64: 1103-1115 (2021)
Takeda Pharmaceutical
Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.
J Med Chem 64: 343-353 (2021)
Galapagos
Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors.
J Med Chem 64: 845-860 (2021)
Arcus Biosciences
Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease.
Eur J Med Chem 212: (2021)
Gazi University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H
Eur J Med Chem 212: (2021)
Zhejiang University
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.
J Med Chem 64: 719-740 (2021)
University Of Cape Town
Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
J Med Chem 64: 566-585 (2021)
University Of Michigan
Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia.
J Nat Prod 84: 1-10 (2021)
The Chinese University Of Hong Kong (Shenzhen)
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer.
Bioorg Med Chem 31: (2021)
Shanghai Institute Of Materia Medica
Synthesis, anticancer and antimicrobial evaluation of new benzofuran based derivatives: PI3K inhibition, quorum sensing and molecular modeling study.
Bioorg Med Chem 31: (2021)
Mansoura University
Development and optimization of halogenated vinyl sulfones as Nrf2 activators for the treatment of Parkinson's disease.
Eur J Med Chem 212: (2021)
Korea Institute Of Science And Technology (Kist)
Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.
Bioorg Med Chem 30: (2021)
Virginia Tech
Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532.
Bioorg Med Chem 30: (2021)
Taisho Pharmaceutical
Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift.
J Med Chem 64: 370-384 (2021)
Seoul National University
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2.
Eur J Med Chem 212: (2021)
Second Military Medical University
Novel amide and imidazole compounds as potent hematopoietic prostaglandin D
Bioorg Med Chem Lett 34: (2021)
Cayman Chemical
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
J Med Chem 64: 385-403 (2021)
East China Normal University
Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of
J Med Chem 64: 481-515 (2021)
Leiden University And Oncode Institute
Spirocyclic Scaffolds in Medicinal Chemistry.
J Med Chem 64: 150-183 (2021)
Goethe University
Novel Nonsecosteroidal Vitamin D Receptor Modulator Combined with Gemcitabine Enhances Pancreatic Cancer Therapy through Remodeling of the Tumor Microenvironment.
J Med Chem 64: 629-643 (2021)
China Pharmaceutical University
Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343.
J Med Chem 64: 861-870 (2021)
Okayama University Graduate School Of Medicine
Development of Orally Efficacious Allosteric Inhibitors of TNF? via Fragment-Based Drug Design.
J Med Chem 64: 417-429 (2021)
Abbvie
3,4-Dihydropyrimidin-2(1
J Med Chem 64: 458-480 (2021)
Universidade De Santiago De Compostela
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
J Med Chem 64: 890-904 (2021)
The State University Of New Jersey
Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis.
J Med Chem 64: 527-542 (2021)
Academia Sinica
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
J Med Chem 64: 677-694 (2021)
Bristol-Myers Squibb Research & Development
Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway.
J Med Chem 64: 797-811 (2021)
University Of Texas At San Antonio
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
J Med Chem 64: 516-526 (2021)
Ochanomizu University
Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue.
J Med Chem 64: 543-565 (2021)
National Institute Of Biological Sciences
Variously substituted 2-oxopyridine derivatives: Extending the structure-activity relationships for allosteric modulation of the cannabinoid CB2 receptor.
Eur J Med Chem 211: (2021)
University Of Pisa
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.
Eur J Med Chem 211: (2021)
Spanish National Cancer Research Centre (Cnio)
Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity.
Eur J Med Chem 211: (2021)
Leipzig University
2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.
Eur J Med Chem 211: (2021)
University Hospital Hradec Kralove
STING, a promising target for small molecular immune modulator: A review.
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
Eur J Med Chem 211: (2021)
Yantai University
Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors.
Eur J Med Chem 211: (2021)
"G. D'Annunzio" University
Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis.
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Design, synthesis and evaluation of PD-L1 peptide antagonists as new anticancer agents for immunotherapy.
Bioorg Med Chem 30: (2021)
Ferdowsi University Of Mashhad
Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
Eur J Med Chem 211: (2021)
Heinrich-Heine-Universit£T D£Sseldorf
Design, synthesis, and biological studies of novel 3-benzamidobenzoic acid derivatives as farnesoid X receptor partial agonist.
Eur J Med Chem 211: (2021)
Guangdong Pharmaceutical University
MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice.
Bioorg Med Chem 30: (2021)
Zhejiang Chinese Medical University
Synthetic approaches to unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles and their MAO-B inhibitory activity. A review.
Bioorg Med Chem 29: (2021)
Medical University-Sofia
Modulators of hERAP2 discovered by high-throughput screening.
Eur J Med Chem 211: (2021)
Institut Pasteur De Lille
Discovery of natural product ellagic acid as a potent CD73 and CD39 dual inhibitor.
Bioorg Med Chem Lett 34: (2021)
Ningxia Medical University
Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma.
Bioorg Med Chem Lett 34: (2021)
Jubilant Therapeutics India
Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases.
Bioorg Med Chem Lett 34: (2021)
Central South University
Novel BuChE-IDO1 inhibitors from sertaconazole: Virtual screening, chemical optimization and molecular modeling studies.
Bioorg Med Chem Lett 34: (2021)
Southwest University
N-(6-phenylpyridazin-3-yl)benzenesulfonamides as highly potent, brain-permeable, and orally active kynurenine monooxygenase inhibitors.
Bioorg Med Chem Lett 33: (2021)
Sumitomo Dainippon Pharma.
Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice.
J Med Chem 64: 812-839 (2021)
University Of Barcelona
Discovery of Venturicidin Congeners and Identification of the Biosynthetic Gene Cluster from
J Nat Prod 84: 110-119 (2021)
Second Military Medical University
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
J Med Chem 64: 1116-1126 (2021)
Second Military Medical University
Tuning the Biological Activity of RGD Peptides with Halotryptophans?.
J Med Chem 64: 586-601 (2021)
Bielefeld University
Phytocannabinoid Pharmacology: Medicinal Properties of
J Nat Prod 84: 142-160 (2021)
Scientus Pharma
Discovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.
J Med Chem 64: 430-439 (2021)
Okayama University Graduate School Of Medicine
Structure-Based Drug Design and Synthesis of PI3K?-Selective Inhibitor (PF-06843195).
J Med Chem 64: 644-661 (2021)
Pfizer
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.
J Med Chem 64: 326-342 (2021)
Pfizer
Development and Therapeutic Potential of NUAKs Inhibitors.
J Med Chem 64: 2-25 (2021)
University Of Science And Technology (Ust)
Bioactive Cyclization Optimizes the Affinity of a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Peptide Inhibitor.
J Med Chem 64: 2523-2533 (2021)
The University Of Queensland
Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
Bioorg Med Chem 30: (2021)
Shandong University
Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
J Med Chem 64: 695-710 (2021)
University Of Hawaii Cancer Center
Natural Products with Potential to Treat RNA Virus Pathogens Including SARS-CoV-2.
J Nat Prod 84: 161-182 (2021)
University Of California San Diego
Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
J Med Chem 64: 602-615 (2021)
Universit£
Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
Bioorg Med Chem Lett 34: (2021)
Shandong First Medical University & Shandong Academy Of Medical Sciences
Elongation of the side chain by linear alkyl groups increases the potency of salacinol, a potent ?-glucosidase inhibitor from the Ayurvedic traditional medicine "Salacia," against human intestinal maltase.
Bioorg Med Chem Lett 33: (2021)
Kindai University
Glycogen Synthase Kinase 3?: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?
J Med Chem 64: 26-41 (2021)
University Of Turin
Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of aldehyde dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy.
Eur J Med Chem 211: (2021)
University Of Michigan
Synthesis and evaluation of tiaprofenic acid-derived UCHL5 deubiquitinase inhibitors.
Bioorg Med Chem 30: (2021)
Wayne State University
In vitro and in vivo effects of inhibitors on actin and myosin.
Bioorg Med Chem 30: (2021)
Tu Dresden
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
Bioorg Med Chem 30: (2021)
China Pharmaceutical University
Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
Eur J Med Chem 211: (2021)
Shandong University
Does targeting Arg98 of FimH lead to high affinity antagonists?
Eur J Med Chem 211: (2021)
University Of Ljubljana
1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase.
Eur J Med Chem 211: (2021)
Palack£
Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold.
Eur J Med Chem 211: (2021)
China Medical University
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.
Bioorg Med Chem Lett 33: (2021)
Shanghai Institute Of Materia Medica
A study of the structure-affinity relationship in SYA16263; is a D
Bioorg Med Chem 30: (2021)
Florida A&M University
Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion.
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Mining Natural Products for Macrocycles to Drug Difficult Targets.
J Med Chem 64: 1054-1072 (2021)
Uppsala University
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
ACS Med Chem Lett 11: 2519-2525 (2020)
Astrazeneca
Novel Tricyclic Pyroglutamide Derivatives as Potent ROR?t Inverse Agonists Identified using a Virtual Screening Approach.
ACS Med Chem Lett 11: 2510-2518 (2020)
Bristol Myers Squibb
Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB
ACS Med Chem Lett 11: 2504-2509 (2020)
Janssen Research & Development
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.
ACS Med Chem Lett 11: 2476-2483 (2020)
Merck
Optimization of Versatile Oxindoles as Selective PI3K? Inhibitors.
ACS Med Chem Lett 11: 2461-2469 (2020)
Merck
Human Insulin-like Peptide 5 (INSL5). Identification of a Simplified Version of Two-Chain Analog A13.
ACS Med Chem Lett 11: 2455-2460 (2020)
The University Of Melbourne
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive
ACS Med Chem Lett 11: 2446-2454 (2020)
The Ohio State University
Decreasing HepG2 Cytotoxicity by Lowering the Lipophilicity of Benzo[d]oxazolephosphinate Ester Utrophin Modulators.
ACS Med Chem Lett 11: 2421-2427 (2020)
University Of Oxford
Synthesis, Characterization, and
ACS Med Chem Lett 11: 2397-2405 (2020)
Bahauddin Zakariya University
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1? Inhibitory Activity.
ACS Med Chem Lett 11: 2389-2396 (2020)
Paraza Pharma
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.
ACS Med Chem Lett 11: 2374-2381 (2020)
Aurigene Discovery Technologies
Novel Compounds as STING Modulators for Treating Hepatitis B Virus Infections.
ACS Med Chem Lett 11: 2372-2373 (2020)
Smith, Gambrell & Russell
Novel Arginase Inhibitors for Treating Cancer and Respiratory Inflammatory Diseases.
ACS Med Chem Lett 11: 2370-2371 (2020)
Smith, Gambrell & Russell
Novel KIF18A Inhibitors for Treating Cancer.
ACS Med Chem Lett 11: 2368-2369 (2020)
Smith, Gambrell & Russell
Carboxamides as Modulators of Sodium Channels.
ACS Med Chem Lett 11: 2364-2365 (2020)
Temple University School Of Pharmacy
Estrogen Receptor Degrading PROTACS for the Treatment of Breast Cancer.
ACS Med Chem Lett 11: 2361-2363 (2020)
Usona Institute
Novel Potassium Channel Inhibitors.
ACS Med Chem Lett 11: 2357-2358 (2020)
Temple University
2-Amino-N-heteroaryl-nicotimamides as Na
ACS Med Chem Lett 11: 2354-2356 (2020)
Temple University School Of Pharmacy
Novel APOL1 Inhibitors for Treating Kidney Diseases.
ACS Med Chem Lett 11: 2352-2353 (2020)
Smith, Gambrell & Russell
Novel CDK2 Inhibitors for Treating Cancer.
ACS Med Chem Lett 11: 2346-2347 (2020)
Smith, Gambrell & Russell
Novel Pyrido-pyrimidinones and Pteridinones as Endoribonuclease Inositol Requiring Enzyme 1 (IRE1?) Inhibitors for Treating Cancer.
ACS Med Chem Lett 11: 2344-2345 (2020)
Smith, Gambrell & Russell
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H
Bioorg Med Chem 30: (2021)
Universidade Federal De S£O Paulo
Identification of N-acyl-N-indanyl-?-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.
Bioorg Med Chem 30: (2021)
Kissei Pharmaceutical
Development of Mcl-1 inhibitors for cancer therapy.
Eur J Med Chem 210: (2021)
National University Of Ireland Galway
Discovery and optimization of substituted oxalamides as novel heme-displacing IDO1 inhibitors.
Bioorg Med Chem Lett 33: (2021)
Phenex Pharmaceuticals
Discovery of BAZ1A bromodomain inhibitors with the aid of virtual screening and activity evaluation.
Bioorg Med Chem Lett 33: (2021)
Sichuan Provincial People'S Hospital
Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis.
J Med Chem 64: 871-889 (2021)
China Pharmaceutical University
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.
ACS Med Chem Lett 11: 2433-2440 (2020)
University Of Ljubljana
Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase.
Eur J Med Chem 209: (2021)
University Of Perugia
Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT
Eur J Med Chem 209: (2021)
Polish Academy Of Sciences
Discovery and development of selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors.
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Isolation and Pharmacological Characterization of Six Opioidergic
J Nat Prod 84: 71-80 (2021)
University Of Illinois At Chicago
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent ?4?2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the ?3?4 Subtype.
J Med Chem 63: 15668-15692 (2020)
Universit£
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPAR?/? Modulators.
J Med Chem 63: 16012-16027 (2020)
Seoul National University
The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist.
Eur J Med Chem 210: (2021)
The University Of Sydney
-Benzyl-linoleamide, a Constituent of
J Nat Prod 83: 3689-3697 (2020)
University Of California Davis
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.
Bioorg Med Chem 29: (2021)
University Of Sharjah
Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: Towards adenosine A
Eur J Med Chem 210: (2021)
Sun Yat-Sen University
Discovery of a novel small-molecule inhibitor of Fam20C that induces apoptosis and inhibits migration in triple negative breast cancer.
Eur J Med Chem 210: (2021)
Southwest Jiaotong University
Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents.
Bioorg Med Chem Lett 33: (2021)
Wenzhou Medical University
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.
Bioorg Med Chem Lett 33: (2021)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
Bioorg Med Chem Lett 33: (2021)
University Of Mysore
Discovery of highly potent heme-displacing IDO1 inhibitors based on a spirofused bicyclic scaffold.
Bioorg Med Chem Lett 33: (2021)
Phenex Pharmaceuticals
Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239.
J Med Chem 63: 15864-15882 (2020)
Idorsia Pharmaceuticals
Cyclic Peptidyl Inhibitors against CAL/CFTR Interaction for Treatment of Cystic Fibrosis.
J Med Chem 63: 15773-15784 (2020)
The Ohio State University
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and
J Med Chem 63: 15906-15945 (2020)
Texas A&M University
The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
Bioorg Med Chem 29: (2021)
Duquesne University
Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells.
Eur J Med Chem 210: (2021)
University Of Sharjah
Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity.
Eur J Med Chem 210: (2021)
Universidad Complutense
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
Eur J Med Chem 210: (2021)
Normandie Univ
Research progress in biological activities of isochroman derivatives.
Eur J Med Chem 210: (2021)
Shaanxi University Of Chinese Medicine
Xanthenes in Medicinal Chemistry - Synthetic strategies and biological activities.
Eur J Med Chem 210: (2021)
Ciimar
N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
Bioorg Med Chem 29: (2021)
Uppsala University
Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.
Eur J Med Chem 213: (2021)
China Pharmaceutical University
Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRAS
Eur J Med Chem 213: (2021)
Shanghai Institute Of Materia Medica (Simm)
Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2Y
J Med Chem 63: 15752-15772 (2020)
Shenyang Pharmaceutical University
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
J Med Chem 63: 15564-15590 (2020)
Astrazeneca
Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors.
Eur J Med Chem 212: (2021)
Ege University
Discovery of indazole-pyridinone derivatives as a novel class of potent and selective MNK1/2 kinase inhibitors that protecting against endotoxin-induced septic shock.
Eur J Med Chem 213: (2021)
Ryvu Therapeutics
Discovery of a Potent and Selective PI3K? Inhibitor (
J Med Chem 63: 14700-14723 (2020)
Lupin
Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors.
J Med Chem 63: 15852-15863 (2020)
Sun Yat-Sen University
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.
J Med Chem 63: 16028-16042 (2020)
Huazhong University Of Science & Technology
Soluble Guanylate Cyclase Inhibitors Discovered among Natural Compounds.
J Nat Prod 83: 3642-3651 (2020)
Inserm U1182 - Cnrs Umr7645
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.
J Med Chem 63: 15821-15851 (2020)
Fondazione Istituto Italiano Di Tecnologia
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
J Med Chem 63: 15410-15448 (2020)
The Ohio State University
Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1.
J Med Chem 63: 15639-15654 (2020)
The Scripps Research Institute
Synthesis and biological evaluation of all possible inosine-mixed cyclic dinucleotides that activate different hSTING variants.
Bioorg Med Chem 29: (2021)
Nankai University
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.
Bioorg Med Chem 29: (2021)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Discovery of a benzimidazole series as the first highly potent and selective ACSL1 inhibitors.
Bioorg Med Chem Lett 33: (2021)
Shionogi Pharmaceutical Research Center
Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.
J Med Chem 63: 15883-15905 (2020)
Icahn School Of Medicine At Mount Sinai
A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors
ChemMedChem (2020)
Texas A&M University
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
J Med Chem 63: 15344-15370 (2020)
Northwestern University
Discovery of novel CA-4 analogs as dual inhibitors of tubulin polymerization and PD-1/PD-L1 interaction for cancer treatment.
Eur J Med Chem 213: (2021)
Southern Medical University
Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-
J Med Chem 63: 15979-15996 (2020)
Zhengzhou University
Optimization of novel oxidative DIMs as Nur77 modulators of the Nur77-Bcl-2 apoptotic pathway.
Eur J Med Chem 211: (2021)
Xiamen University
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
Eur J Med Chem 213: (2021)
Shandong University
Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents.
Eur J Med Chem 212: (2021)
Xuzhou Medical University
4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines.
J Med Chem 63: 15603-15620 (2020)
Albert-Ludwigs-Universit£T Freiburg
Design, synthesis, evaluation, and SAR of 4-phenylindoline derivatives, a novel class of small-molecule inhibitors of the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) interaction.
Eur J Med Chem 211: (2021)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Discovery of tetrahydroquinolines and benzomorpholines as novel potent ROR?t agonists.
Eur J Med Chem 211: (2021)
Fudan University
Recent Advances in the Development of PD-L1 Modulators: Degraders, Downregulators, and Covalent Inhibitors.
J Med Chem 63: 15389-15398 (2020)
Southern Medical University
Identification and structure-activity relationship studies of small molecule inhibitors of the human cathepsin D.
Bioorg Med Chem 29: (2021)
Aten Porus Lifesciences
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
J Med Chem 63: 15709-15725 (2020)
Lanzhou University
Heteroaryl ether analogues of an antileishmanial 7-substituted 2-nitroimidazooxazine lead afford attenuated hERG risk: In vitro and in vivo appraisal.
Eur J Med Chem 209: (2021)
University Of Auckland
Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists.
J Med Chem 63: 15399-15409 (2020)
Chinese Academy Of Sciences
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
J Med Chem 63: 15541-15563 (2020)
TBA
Discovery of Novel and Highly Potent Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment.
J Med Chem 63: 15946-15959 (2020)
Southern Medical University
Structural modifications in the distal, regulatory region of histamine H
Eur J Med Chem 213: (2021)
Jagiellonian University Medical College
Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
Eur J Med Chem 213: (2021)
Sichuan University
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNF? Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.
J Med Chem 63: 15050-15071 (2020)
Bristol Myers Squibb
ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors.
Bioorg Med Chem Lett 33: (2021)
Vertex Pharmaceuticals
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
J Med Chem 63: 14885-14904 (2020)
Novartis Institutes For Biomedical Research
Paracetamol analogues conjugated by FAAH induce TRPV1-mediated antinociception without causing acute liver toxicity.
Eur J Med Chem 213: (2021)
Lund University
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
Eur J Med Chem 209: (2021)
Nankai University
-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
J Med Chem 63: 14921-14936 (2020)
West China Hospital Of Sichuan University
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.
Bioorg Med Chem 29: (2021)
University Of S£O Paulo
Lead optimization of the VU0486321 series of mGlu
Bioorg Med Chem Lett 32: (2021)
Vanderbilt University
Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology.
Bioorg Med Chem Lett 32: (2021)
Amgen
Store-Operated Calcium Entry as a Therapeutic Target in Acute Pancreatitis: Discovery and Development of Drug-Like SOCE Inhibitors.
J Med Chem 63: 14761-14779 (2020)
Universit£
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
J Nat Prod 83: 3571-3583 (2020)
Hospitales Universitarios De Granada/University Of Granada
Discovery of Potent, Highly Selective, and
J Med Chem 63: 14576-14593 (2020)
Novartis Institutes For Biomedical Research
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.
Eur J Med Chem 211: (2021)
Guangzhou Institutes Of Biomedicine And Health
Synthesis and structure-activity studies of novel anhydrohexitol-based Leucyl-tRNA synthetase inhibitors.
Eur J Med Chem 211: (2021)
Ku Leuven
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
Eur J Med Chem 212: (2021)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors.
Bioorg Med Chem 29: (2021)
Chinese Academy Of Medical Sciences & Peking Union Medical College
Discovery of 4-amino-1H-pyrazolo[3,4-d]pyrimidin derivatives as novel discoidin domain receptor 1 (DDR1) inhibitors.
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.
Bioorg Med Chem Lett 31: (2021)
Jiangnan University
Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors.
Bioorg Med Chem Lett 31: (2021)
Central South University
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
Eur J Med Chem 211: (2021)
Panjab University
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.
Eur J Med Chem 210: (2021)
Jiangxi Science & Technology Normal University
Xanthones for melanogenesis inhibition: Molecular docking and QSAR studies to understand their anti-tyrosinase activity.
Bioorg Med Chem 29: (2021)
Universidade Dos A£Ores
Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors.
Bioorg Med Chem Lett 31: (2021)
Zhejiang Hisun Pharmaceutical
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.
Eur J Med Chem 211: (2021)
China Pharmaceutical University
EST64454: a Highly Soluble ?
J Med Chem 63: 14979-14988 (2020)
Esteve Pharmaceuticals
Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective.
Eur J Med Chem 210: (2021)
North-West University
Design and development of FGF-23 antagonists: Definition of the pharmacophore and initial structure-activity relationships probed by synthetic analogues.
Bioorg Med Chem 29: (2021)
Tennessee Technological University
Current status in the discovery of dual BET/HDAC inhibitors.
Bioorg Med Chem Lett 31: (2021)
The First Affiliated Hospital Of Zhengzhou University
Synthesis and evaluation of a UMI-77-based fluorescent probe for selective detecting Mcl-1 protein and imaging in living cancer cells.
Bioorg Med Chem 29: (2021)
Shandong University
Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway.
Eur J Med Chem 211: (2021)
Massachusetts College Of Pharmacy And Health Sciences University
Structure guided development of potent piperazine-derived hydroxamic acid inhibitors targeting falcilysin.
Bioorg Med Chem Lett 32: (2021)
California State University
Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements
J Med Chem 63: 14668-14679 (2020)
Medical University Of Innsbruck
Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection.
J Med Chem 63: 14740-14760 (2020)
Bristol Myers Squibb Research And Early Development
Fragment-to-Lead Medicinal Chemistry Publications in 2019.
J Med Chem 63: 15494-15507 (2020)
Novartis Institutes For Biomedical Research
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.
J Med Chem 63: 14404-14424 (2020)
Jinan University
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.
Bioorg Med Chem 29: (2021)
Hangzhou Xixi Hospital
Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable "click" oxime bond tethers and preclinical evaluation against prostate cancer.
Eur J Med Chem 211: (2021)
University Of Ioannina
Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2.
Eur J Med Chem 211: (2021)
Universit£
Development of pyrimidone D1 dopamine receptor positive allosteric modulators.
Bioorg Med Chem Lett 31: (2021)
National Institutes Of Health
Pyrrolo[2,3-b]pyridine-3-one derivatives as novel fibroblast growth factor receptor 4 inhibitors for the treatment of hepatocellular carcinoma.
Bioorg Med Chem 29: (2021)
Nanjing University Of Chinese Medicine
Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.
Bioorg Med Chem 29: (2021)
Dalian University Of Technology
Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.
Bioorg Med Chem 29: (2021)
University Of Florence
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment.
Eur J Med Chem 211: (2021)
Chinese Academy Of Sciences
Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.
J Med Chem 63: 14680-14699 (2020)
Goethe University Frankfurt
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
J Med Chem 63: 14626-14646 (2020)
University Of North Carolina At Chapel Hill
Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective.
J Med Chem 63: 15115-15139 (2020)
China Pharmaceutical University
Effects of C-Terminal B-Chain Modifications in a Relaxin 3 Agonist Analogue.
ACS Med Chem Lett 11: 2336-2340 (2020)
The University Of Melbourne
Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
ACS Med Chem Lett 11: 2318-2324 (2020)
Virginia Commonwealth University
Simultaneous Inhibition of SIRT2 Deacetylase and Defatty-Acylase Activities via a PROTAC Strategy.
ACS Med Chem Lett 11: 2305-2311 (2020)
Cornell University
In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in
ACS Med Chem Lett 11: 2294-2299 (2020)
Universit£
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
ACS Med Chem Lett 11: 2285-2289 (2020)
University Of Bayreuth
Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium
ACS Med Chem Lett 11: 2277-2284 (2020)
University Of Florence
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation.
ACS Med Chem Lett 11: 2268-2276 (2020)
University Of Siena
Fluorescent Probes for Ecto-5'-nucleotidase (CD73).
ACS Med Chem Lett 11: 2253-2260 (2020)
University Of Bonn
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3K? Inhibitors.
ACS Med Chem Lett 11: 2244-2252 (2020)
Arcus Biosciences
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.
ACS Med Chem Lett 11: 2238-2243 (2020)
Dana-Farber Cancer Institute
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.
ACS Med Chem Lett 11: 2227-2231 (2020)
Janssen Pharmaceutica
?-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs).
ACS Med Chem Lett 11: 2212-2220 (2020)
University Of Copenhagen
Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the ?1?2?2 GABA
ACS Med Chem Lett 11: 2204-2211 (2020)
California Institute Of Technology
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
ACS Med Chem Lett 11: 2195-2203 (2020)
Bristol Myers Squibb Research
Hydrogen Peroxide Inducible JAK3 Covalent Inhibitor: Prodrug for the Treatment of RA with Enhanced Safety Profile.
ACS Med Chem Lett 11: 2182-2189 (2020)
China Pharmaceutical University
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.
ACS Med Chem Lett 11: 2174-2181 (2020)
China Pharmaceutical University
Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer.
ACS Med Chem Lett 11: 2156-2164 (2020)
Temple University
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.
ACS Med Chem Lett 11: 2151-2155 (2020)
Shanghai Hengrui Pharmaceutical
Biotransformation: Impact and Application of Metabolism in Drug Discovery.
ACS Med Chem Lett 11: 2087-2107 (2020)
Hypha Discovery
Novel 5-Alkyl Pyrrolidine Orexin Receptor Agonists for Treating Sleep Disorders.
ACS Med Chem Lett 11: 2085-2086 (2020)
Smith, Gambrell & Russell
Novel KIF18A Inhibitors for Treating Cancer.
ACS Med Chem Lett 11: 2079-2080 (2020)
Smith, Gambrell & Russell
Novel Bicyclic Heteroaryl Compounds as ?-Secretase Modulators for Treating Alzheimer's Disease.
ACS Med Chem Lett 11: 2077-2078 (2020)
Smith, Gambrell & Russell
Therapeutic Potential of Autotaxin Inhibitors in Treatment of Interstitial Lung Diseases.
ACS Med Chem Lett 11: 2075-2076 (2020)
Therachem Research Medilab
Use of Dihydroorotate Dehydrogenase Inhibitors for Treatment of Autoimmune Diseases and Cancer.
ACS Med Chem Lett 11: 2072-2074 (2020)
Therachem Research Medilab
Modulation of Androgen Receptor for Therapeutic Application in Cancer and Viral Infection.
ACS Med Chem Lett 11: 2068-2069 (2020)
Usona Institute
Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.
Bioorg Med Chem 29: (2021)
Kangwon National University
Design, synthesis, and anti-proliferative evaluation of new quinazolin-4(3H)-ones as potential VEGFR-2 inhibitors.
Bioorg Med Chem 29: (2021)
Al-Azhar University
Design, synthesis and biological evaluation of novel chalcone-like compounds as potent and reversible pancreatic lipase inhibitors.
Bioorg Med Chem 29: (2021)
Zhengzhou University
Recent Advances in ?
J Med Chem 63: 15218-15242 (2020)
Shenyang Pharmaceutical University
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
J Med Chem 63: 14780-14804 (2020)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)
Computational Fragment-Based Design Facilitates Discovery of Potent and Selective Monoamine Oxidase-B (MAO-B) Inhibitor.
J Med Chem 63: 15021-15036 (2020)
Sunshine Lake Pharma
Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity.
J Med Chem 63: 14805-14820 (2020)
Taisho Pharmaceutical
Targeted Covalent Inhibition of
ACS Med Chem Lett 11: 2131-2138 (2020)
Broad Institute Of Mit And Harvard
Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging.
J Med Chem 63: 15037-15049 (2020)
Yale University
Design, Synthesis, and Structure-Activity Relationship Studies of (4-Alkoxyphenyl)glycinamides and Bioisosteric 1,3,4-Oxadiazoles as GPR88 Agonists.
J Med Chem 63: 14989-15012 (2020)
Research Triangle Institute
Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions.
J Med Chem 63: 14867-14884 (2020)
Glaxosmithkline
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 63: 14609-14625 (2020)
Institute
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3K? inhibitors via docking-based virtual screening.
Bioorg Med Chem 29: (2021)
Zhejiang University
The discovery of quinoline derivatives, as NF-?B inducing kinase (NIK) inhibitors with anti-inflammatory effects in vitro, low toxicities against T cell growth.
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3).
Eur J Med Chem 210: (2021)
Celon Pharma
Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation.
Eur J Med Chem 212: (2021)
University Of Siena
Water-soluble inhibitors of ABCG2 (BCRP) - A fragment-based and computational approach.
Eur J Med Chem 210: (2021)
University Of Regensburg
From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4).
Eur J Med Chem 210: (2021)
Eberhard Karls Universit£T T£Bingen
Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior.
J Med Chem 63: 13951-13972 (2020)
University Of Texas Medical Branch
Targeting the Allosteric Pathway That Interconnects the Core-Functional Scaffold and the Distal Phosphorylation Sites for Specific Dephosphorylation of Bcl-2.
J Med Chem 63: 13733-13744 (2020)
Dalian University Of Technology
Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.
J Med Chem 63: 14017-14044 (2020)
Janssen-Cilag
High Selectivity of an ?-Conotoxin LvIA Analogue for ?3?2 Nicotinic Acetylcholine Receptors Is Mediated by ?2 Functionally Important Residues.
J Med Chem 63: 13656-13668 (2020)
Guangxi University
Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors.
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors.
Bioorg Med Chem 29: (2021)
Jadavpur University
An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
Eur J Med Chem 210: (2021)
University Of Kwazulu-Natal (Westville)
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure?.
J Med Chem 64: 357-369 (2021)
Vrije Universiteit Brussel
Discovery of a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins through the modulation of atropisomer interconversion properties.
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.
Bioorg Med Chem Lett 31: (2021)
Shanghai Institute Of Pharmaceutical Industry
ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker.
Eur J Med Chem 212: (2021)
Southeast University
2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents.
Eur J Med Chem 210: (2021)
China Medical University
Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations.
Eur J Med Chem 210: (2021)
Csir-Indian Institute Of Chemical Biology
PROTACs to address the challenges facing small molecule inhibitors.
Eur J Med Chem 210: (2021)
Oregon Health & Science University
Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase.
Eur J Med Chem 210: (2021)
Comsats University Islamabad
Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3.
Eur J Med Chem 210: (2021)
Ludwig-Maximilians University
Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities.
J Med Chem 65: 2716-2746 (2022)
University Of Naples "Federico Ii
Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo.
J Med Chem 63: 13825-13850 (2020)
National Engineering Research Center For The Emergency Drug
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.
J Med Chem 64: 941-957 (2021)
Fudan University
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
J Med Chem 63: 13994-14016 (2020)
University Of Michigan
Novel naphthylamide derivatives as dual-target antifungal inhibitors: Design, synthesis and biological evaluation.
Eur J Med Chem 210: (2021)
Liaocheng University
Syntheses and anti-HIV and human cluster of differentiation 4 (CD4) down-modulating potencies of pyridine-fused cyclotriazadisulfonamide (CADA) compounds.
Bioorg Med Chem 28: (2020)
University Of Nevada
Discovery of (
J Med Chem 63: 13973-13993 (2020)
Hefei Institutes Of Physical Science
Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer.
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Novel 2,7-Diazaspiro[4,4]nonane Derivatives to Inhibit Mouse and Human Osteoclast Activities and Prevent Bone Loss in Ovariectomized Mice without Affecting Bone Formation.
J Med Chem 63: 13680-13694 (2020)
Universit£
Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.
J Med Chem 63: 14087-14117 (2020)
National Cancer Institute
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT
Bioorg Med Chem Lett 31: (2021)
Janssen Research & Development
Synthesis and Pharmacology of a Novel ?-? Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.
J Med Chem 63: 13618-13637 (2020)
St Louis College Of Pharmacy And Washington University
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
J Med Chem 63: 13796-13824 (2020)
Merck
Therapeutic potential for coxibs-nitric oxide releasing hybrids in cystic fibrosis.
Eur J Med Chem 210: (2021)
Sapienza University Of Rome
Discovery of novel pyrazolo[3,4-b]pyridine scaffold-based derivatives as potential PIM-1 kinase inhibitors in breast cancer MCF-7 cells.
Bioorg Med Chem 28: (2020)
Suez Canal University
Design, synthesis and biological evaluation of new bivalent quinazoline analogues as IAP antagonists.
Bioorg Med Chem Lett 34: (2021)
Chung-Ang University
4-(Difluoromethyl)-5-(4-((3
J Med Chem 63: 13595-13617 (2020)
University Of Basel
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores.
Bioorg Med Chem Lett 32: (2021)
Merck
Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.
Eur J Med Chem 210: (2021)
Iranian Fisheries Science Research Institute
N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay.
Bioorg Med Chem 28: (2020)
Entasis Therapeutics
Development of autotaxin inhibitors: A series of tetrazole cinnamides.
Bioorg Med Chem Lett 31: (2021)
Novartis Institutes For Biomedical Research
Design, synthesis and screening of benzimidazole containing compounds with methoxylated aryl radicals as cytotoxic molecules on (HCT-116) colon cancer cells.
Eur J Med Chem 209: (2021)
Misr University For Science & Technology
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.
Eur J Med Chem 210: (2021)
Shandong First Medical University & Shandong Academy Of Medical Sciences
Synthesis and biological screening of thiosemicarbazones of substituted 3-acetylcoumarins having d-glucose moiety.
Bioorg Med Chem Lett 30: (2020)
Institute For Advanced Technology (Vietnam Academy Of Military Science And Technology)
Recent research progress of Uncaria spp. based on alkaloids: phytochemistry, pharmacology and structural chemistry.
Eur J Med Chem 210: (2021)
China Pharmaceutical University
In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition.
Eur J Med Chem 210: (2021)
Universit£
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.
Eur J Med Chem 210: (2021)
Hunan University Of Science And Technology
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine
J Med Chem 63: 13878-13898 (2020)
University Of Kansas
Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor.
J Med Chem 63: 13762-13795 (2020)
Servier Research Institute Of Medicinal Chemistry
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
Eur J Med Chem 209: (2021)
National Institute Of Pharmaceutical Education And Research (Niper) - Ahmedabad
Peptide Inhibitors of the ?-Cobratoxin-Nicotinic Acetylcholine Receptor Interaction.
J Med Chem 63: 13709-13718 (2020)
University Of Bergen
Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models.
J Med Chem 63: 14905-14920 (2020)
Korea Basic Science Institute (Kbsi)
A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor ? Binding Properties and Biological Activities.
J Med Chem 63: 13124-13139 (2020)
Aix Marseille University
Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions.
J Med Chem 63: 13187-13196 (2020)
University Of South Florida
Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis.
Eur J Med Chem 210: (2021)
Centro De Investigaciones Biol�Gicas Margarita Salas-Csic
Di-aryl guanidinium derivatives: Towards improved ?2-Adrenergic affinity and antagonist activity.
Eur J Med Chem 209: (2021)
Trinity College
Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?
Eur J Med Chem 210: (2021)
University Of Patras
Small molecule therapeutics for tauopathy in Alzheimer's disease: Walking on the path of most resistance.
Eur J Med Chem 209: (2021)
Karolinska Institutet
Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation.
Bioorg Med Chem Lett 30: (2020)
Xinyang Normal University
Discovery of a Remarkable Methyl Shift Effect in the Vanilloid Activity of Triterpene Amides.
J Nat Prod 83: 3476-3481 (2020)
National Research Council (Icb-Cnr)
Synthetic Lethality through the Lens of Medicinal Chemistry.
J Med Chem 63: 14151-14183 (2020)
Istituto Italiano Di Tecnologia
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
Bioorg Med Chem Lett 30: (2020)
Xuzhou Medical University
The optimization of a novel selective antagonist for human M
Bioorg Med Chem Lett 30: (2020)
Shanghai Jiao Tong University School Of Medicine
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives.
Bioorg Med Chem Lett 30: (2020)
Shionogi
Sulfonamide antibiotics inhibit RNAi by binding to human Argonaute protein 2 PAZ.
Bioorg Med Chem Lett 30: (2020)
Gifu University
An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.
Eur J Med Chem 210: (2021)
Jamia Millia Islamia (A Central University)
Synthesis and evaluation of HIF-1? inhibitory activities of novel panaxadiol derivatives.
Bioorg Med Chem Lett 30: (2020)
Yanbian University
Synthesis and biological activities of simplified aplysiatoxin analogs focused on the CH/? interaction.
Bioorg Med Chem Lett 30: (2020)
Kyoto University
The food-grade antimicrobial xanthorrhizol targets the enoyl-ACP reductase (FabI) in Escherichia coli.
Bioorg Med Chem Lett 30: (2020)
Yonsei University
Design, synthesis, and computational validation of novel compounds selectively targeting HER2-expressing breast cancer.
Bioorg Med Chem Lett 30: (2020)
Bristol University
Discovery of natural TRPA1 activators through pharmacophore-based virtual screening and a biological assay.
Bioorg Med Chem Lett 31: (2021)
Kyoto University Shogoin-Kawaharacho
Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth invitro and invivo.
Eur J Med Chem 210: (2021)
East China University Of Science And Technology
An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
Eur J Med Chem 209: (2021)
University Of Bari "Aldo Moro
Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.
Eur J Med Chem 209: (2021)
Key Laboratory Of Technology Of Drug Preparation (Zhengzhou University)
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.
Bioorg Med Chem 28: (2020)
University Of Oxford
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
Bioorg Med Chem Lett 30: (2020)
Dalian Institute Of Chemical Physics
Structure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer.
J Nat Prod 84: 797-813 (2021)
Bc Cancer
5-Phenyl-1,3,4-oxadiazol-2(3
J Med Chem 63: 12942-12956 (2020)
University College London
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
Eur J Med Chem 209: (2021)
Isf College Of Pharmacy
Pyridine alkaloids with activity in the central nervous system.
Bioorg Med Chem 28: (2020)
University Of Auckland
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.
Bioorg Med Chem 28: (2020)
Lupin
Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma.
J Med Chem 63: 12707-12724 (2020)
Universit£
Proposed Allosteric Inhibitors Bind to the ATP Site of CK2?.
J Med Chem 63: 12786-12798 (2020)
University Of Cambridge
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
J Med Chem 63: 12957-12977 (2020)
The University Of Texas Md Anderson Cancer Center
Discovery of a Beetroot Protease Inhibitor to Identify and Classify Plant-Derived Cystine Knot Peptides.
J Nat Prod 83: 3305-3314 (2020)
Medical University Of Vienna
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
J Med Chem 63: 15187-15217 (2020)
Soochow University
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Eur J Med Chem 209: (2021)
Chinese Academy Of Sciences
Design, synthesis and bioevaluation of inhibitors targeting HSP90-CDC37 protein-protein interaction based on a hydrophobic core.
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Design, synthesis, biological activity evaluation of 3-(4-phenyl-1H-imidazol-2-yl)-1H-pyrazole derivatives as potent JAK 2/3 and aurora A/B kinases multi-targeted inhibitors.
Eur J Med Chem 209: (2021)
Xuzhou Medical University
Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
J Med Chem 63: 12574-12594 (2020)
Bayer
Therapeutic Targeting of MMP-12 for the Treatment of Chronic Obstructive Pulmonary Disease.
J Med Chem 63: 12911-12920 (2020)
University Of California Riverside
[1,2,4]Triazolo[1,5-
J Med Chem 63: 12887-12910 (2020)
Janssen Pharmaceutica N. V.
Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and
J Med Chem 63: 13013-13030 (2020)
University Of Cape Town
Identification, Structure-Activity Relationships of Marine-Derived Indolocarbazoles, and a Dual PKC?/? Inhibitor with Potent Antipancreatic Cancer Efficacy.
J Med Chem 63: 12978-12991 (2020)
Zhejiang University
PROTACs suppression of GSK-3?, a crucial kinase in neurodegenerative diseases.
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Synthesis and identification of a novel derivative of salidroside as a selective, competitive inhibitor of monoamine oxidase B with enhanced neuroprotective properties.
Eur J Med Chem 209: (2021)
Fujian University Of Traditional Chinese Medicine
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Bioorg Med Chem Lett 31: (2021)
Bristol-Myers Squibb
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.
Bioorg Med Chem Lett 30: (2020)
Sanofi
Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.
J Med Chem 63: 12642-12665 (2020)
University Of Tennessee Health Science Center
Structure-Activity Relationships of Noncovalent Immunoproteasome ?5i-Selective Dipeptides.
J Med Chem 63: 13103-13123 (2020)
Weill Cornell Medicine
Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone.
J Med Chem 63: 13064-13075 (2020)
University Of Florida
Structural Insights into the Recognition of Mono- and Diacetylated Histones by the ATAD2B Bromodomain.
J Med Chem 63: 12799-12813 (2020)
Albany College Of Pharmacy And Health Sciences
An update into the medicinal chemistry of translocator protein (TSPO) ligands.
Eur J Med Chem 209: (2021)
University Of Pisa
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II ? over ?.
J Med Chem 63: 12873-12886 (2020)
Istituto Italiano Di Tecnologia
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
Eur J Med Chem 209: (2021)
Shanghai Institute Of Materia Medica
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Eur J Med Chem 209: (2021)
Menoufia University
Targeting Atg4B for cancer therapy: Chemical mediators.
Eur J Med Chem 209: (2021)
Sichuan University
Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.
Eur J Med Chem 209: (2021)
The University Of Tours
Design, synthesis and biological assessment of new selective COX-2 inhibitors including methyl sulfonyl moiety.
Eur J Med Chem 209: (2021)
Anadolu University
SP1-independent inhibition of FOXM1 by modified thiazolidinediones.
Eur J Med Chem 209: (2021)
University Of Alberta
Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker.
Bioorg Med Chem 28: (2020)
Johns Hopkins University
Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations.
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
Bioorg Med Chem 28: (2020)
Beijing Institute Of Technology
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Synthesis, biological evaluation and in silico modeling of novel pan-genotypic NS5A inhibitors.
Bioorg Med Chem 28: (2020)
Chemical Diversity Research Institute
Rational design of cell-permeable cyclic peptides containing a d-Pro-l-Pro motif.
Bioorg Med Chem 28: (2020)
The Ohio State University
Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-?-hydroxylase.
Bioorg Med Chem 28: (2020)
University Of Oxford
Discovery of heterocycle-containing ?-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors.
Eur J Med Chem 209: (2021)
Shanghai Jiao Tong University
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.
Bioorg Med Chem 28: (2020)
Mansoura University
Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility.
Bioorg Med Chem 28: (2020)
Northeastern University
Next generation quorum sensing inhibitors: Accounts on structure activity relationship studies and biological activities.
Bioorg Med Chem 28: (2020)
Dnyanprassarak Mandal'S College And Research Centre
Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction.
Bioorg Med Chem 28: (2020)
Irbm
Design and synthesis of new disubstituted benzoxazolone derivatives that act as iNOS inhibitors with potent anti-inflammatory activity against LPS-induced acute lung injury (ALI).
Bioorg Med Chem 28: (2020)
Shanxi Medical University
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity.
Bioorg Med Chem 28: (2020)
Daiichi Sankyo
Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model.
Eur J Med Chem 209: (2021)
Sichuan University
Discovery of EST73502, a Dual ?-Opioid Receptor Agonist and ?
J Med Chem 63: 15508-15526 (2020)
Esteve Pharmaceuticals
Backbone Cyclization Turns a Venom Peptide into a Stable and Equipotent Ligand at Both Muscle and Neuronal Nicotinic Receptors.
J Med Chem 63: 12682-12692 (2020)
Universit£
Discovery of Tricyclic Xanthines as Agonists of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18.
ACS Med Chem Lett 11: 2024-2031 (2020)
University Of Bonn
Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity.
ACS Med Chem Lett 11: 2017-2023 (2020)
Fuji Yakuhin
Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders.
ACS Med Chem Lett 11: 2010-2016 (2020)
Sanofi R&D
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
ACS Med Chem Lett 11: 2002-2009 (2020)
Janssen Research & Development
De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits.
ACS Med Chem Lett 11: 1993-2001 (2020)
Msd
Discovery of a Cyclic Choline Analog That Inhibits Anaerobic Choline Metabolism by Human Gut Bacteria.
ACS Med Chem Lett 11: 1980-1985 (2020)
Harvard University
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
ACS Med Chem Lett 11: 1965-1972 (2020)
Purdue University
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine D
ACS Med Chem Lett 11: 1956-1964 (2020)
National Institute On Drug Abuse-Intramural Research Program
Mechanism-Based Design of 3-Amino-4-Halocyclopentenecarboxylic Acids as Inactivators of GABA Aminotransferase.
ACS Med Chem Lett 11: 1949-1955 (2020)
Northwestern University
Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A
ACS Med Chem Lett 11: 1935-1941 (2020)
National Institute Of Diabetes And Digestive And Kidney Disease
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies.
ACS Med Chem Lett 11: 1928-1934 (2020)
Rwth Aachen University
Gibberellin JRA-003: A Selective Inhibitor of Nuclear Translocation of IKK?.
ACS Med Chem Lett 11: 1913-1918 (2020)
University Of Michigan
Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma.
ACS Med Chem Lett 11: 1899-1904 (2020)
Bristol Myers Squibb
Dethioacylation by Sirtuins 1-3: Considerations for Drug Design Using Mechanism-Based Sirtuin Inhibition.
ACS Med Chem Lett 11: 1886-1892 (2020)
University Of Copenhagen
Harmaline Analogs as Substrate-Selective Cyclooxygenase-2 Inhibitors.
ACS Med Chem Lett 11: 1881-1885 (2020)
Vanderbilt University School Of Medicine
Discovery and Evaluation of Pyrazolo[3,4-
ACS Med Chem Lett 11: 1863-1868 (2020)
Hubei Bio-Pharmaceutical Industrial Technological Institute
Synthesis and SAR Studies of 1
ACS Med Chem Lett 11: 1848-1854 (2020)
University Of Nebraska Medical Center
Inhibition of Macrophage Migration Inhibitory Factor by a Chimera of Two Allosteric Binders.
ACS Med Chem Lett 11: 1843-1847 (2020)
L2 Diagnostics
Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.
ACS Med Chem Lett 11: 1837-1842 (2020)
Vanderbilt University School Of Medicine
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X
ACS Med Chem Lett 11: 1829-1836 (2020)
Abbvie
The Resurrection of Phenotypic Drug Discovery.
ACS Med Chem Lett 11: 1820-1828 (2020)
Temple University School Of Pharmacy
Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.
ACS Med Chem Lett 11: 1810-1819 (2020)
Therapeutics
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
ACS Med Chem Lett 11: 1799-1809 (2020)
University Of California, Los Angeles
Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome.
ACS Med Chem Lett 11: 1795-1796 (2020)
Usona Institute
Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion.
Eur J Med Chem 209: (2021)
Universit£
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.
J Med Chem 63: 14562-14575 (2020)
Cullgen (Shanghai)
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
J Med Chem 63: 14382-14403 (2020)
China Pharmaceutical University
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
J Med Chem 63: 12725-12747 (2020)
Pfizer
Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3
J Med Chem 63: 14502-14521 (2020)
TBA
Design, Synthesis, and Pharmacological Evaluation of Analogues Derived from the PLEV Tetrapeptide as Protein-Protein Interaction Modulators of Voltage-Gated Sodium Channel 1.6.
J Med Chem 63: 11522-11547 (2020)
TBA
Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective ?
Eur J Med Chem 209: (2021)
Guangdong Medical University
Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator.
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
Eur J Med Chem 209: (2021)
University Of Pisa
Current development of CBP/p300 inhibitors in the last decade.
Eur J Med Chem 209: (2021)
Zhengzhou University
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase.
J Med Chem 63: 11498-11521 (2020)
Goethe-University Of Frankfurt
Design, synthesis and biological evaluation of novel naphthoquinone-4-aminobenzensulfonamide/carboxamide derivatives as proteasome inhibitors.
Eur J Med Chem 209: (2021)
Ege University
Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer.
Eur J Med Chem 209: (2021)
Texas Tech University Health Sciences Center
Rapid discovery of a selective butyrylcholinesterase inhibitor using structure-based virtual screening.
Bioorg Med Chem Lett 30: (2020)
The University Of Queensland
Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis.
Eur J Med Chem 209: (2021)
Egyptian Russian University
The discovery of potent small molecule activators of human STING.
Eur J Med Chem 209: (2021)
Curadev Pharma
Crystal structure of Leishmania mexicana cysteine protease B in complex with a high-affinity azadipeptide nitrile inhibitor.
Bioorg Med Chem 28: (2020)
University Of S£O Paulo
hDM2 protein-binding peptides screened from stapled ?-helical peptide phage display libraries with different types of staple linkers.
Bioorg Med Chem Lett 30: (2020)
Tokyo Institute Of Technology
Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Squaric acid analogues in medicinal chemistry.
Eur J Med Chem 209: (2021)
Palacky University Olomouc
Selective targeting of the ?C and DFG-out pocket in p38 MAPK.
Eur J Med Chem 208: (2020)
Johann Wolfgang Goethe University
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).
Bioorg Med Chem Lett 30: (2020)
Luoxin Pharmaceutical (Shanghai) Co.
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
J Med Chem 63: 14522-14529 (2020)
Fount Therapeutics
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors.
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Meroterpenoids produced by fungi: Occurrence, structural diversity, biological activities, and their molecular targets.
Eur J Med Chem 209: (2021)
Guangzhou University Of Chinese Medicine
Structure activity relationship of novel antiviral nucleosides against Enterovirus A71.
Bioorg Med Chem Lett 30: (2020)
National Institute Of Diabetes And Digestive And Kidney Disease
Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma.
J Med Chem 63: 11484-11497 (2020)
University Of Southern California
Biological Evaluation of Selected Flavonoids as Inhibitors of MNKs Targeting Acute Myeloid Leukemia.
J Nat Prod 83: 2967-2975 (2020)
The Chinese University Of Hong Kong (Shenzhen)
Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.
J Nat Prod 83: 3041-3049 (2020)
Nantong University
Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
J Med Chem 63: 14470-14501 (2020)
Zhejiang University
New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
Eur J Med Chem 209: (2021)
Palack£
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
J Med Chem 63: 12083-12099 (2020)
Shandong University
Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3? inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents.
Eur J Med Chem 209: (2021)
Anhui Medical University
Automated Design of Macrocycles for Therapeutic Applications: From Small Molecules to Peptides and Proteins.
J Med Chem 63: 12100-12115 (2020)
Schrodinger
Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors.
Bioorg Med Chem Lett 30: (2020)
Key Laboratory Of Molecule Synthesis And Function Discovery (Fujian Province University)
Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Eur J Med Chem 207: (2020)
University Of Auckland
Design, synthesis and biological evaluation of indanone-chalcone hybrids as potent and selective hCES2A inhibitors.
Eur J Med Chem 209: (2021)
Shanghai University Of Traditional Chinese Medicine
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.
Bioorg Med Chem 28: (2020)
Indian Institute Of Technology (Banaras Hindu University)
Druggable targets from coronaviruses for designing new antiviral drugs.
Bioorg Med Chem 28: (2020)
Federal University Of Alagoas
N-phenyl ureidobenzenesulfonates, a novel class of promising human dihydroorotate dehydrogenase inhibitors.
Bioorg Med Chem 28: (2020)
Universit£
Design and synthesis of Coenzyme A analogues as Aurora kinase A inhibitors: An exploration of the roles of the pyrophosphate and pantetheine moieties.
Bioorg Med Chem 28: (2020)
University College London
Preparation and evaluation of soluble epoxide hydrolase inhibitors with improved physical properties and potencies for treating diabetic neuropathic pain.
Bioorg Med Chem 28: (2020)
Synthia
Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators.
Bioorg Med Chem 28: (2020)
University Of California
Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.
Bioorg Med Chem 28: (2020)
Universit£T M£Nster
Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase.
Bioorg Med Chem 28: (2020)
Bristol Myers Squibb
Analogs of nitrofuran antibiotics are potent GroEL/ES inhibitor pro-drugs.
Bioorg Med Chem 28: (2020)
Indiana University School Of Medicine
Dual antagonists of ?5?1/?v?1 integrin for airway hyperresponsiveness.
Bioorg Med Chem Lett 30: (2020)
University Of California San Francisco
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.
Bioorg Med Chem Lett 30: (2020)
Janssen Pharmaceutical Research & Development
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
Eur J Med Chem 207: (2020)
South China Agricultural University
The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis.
Eur J Med Chem 208: (2020)
University Of Pisa
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