PMID
Article Title
Citation
Organization
Download
View Data
Discovery of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one and 3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one derivatives as novel ENPP1 inhibitors.
Bioorg Med Chem Lett 75: (2022)
Korea Institute of Science and Technology
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
J Med Chem 65: 11726-11744 (2022)
Saarland University
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
J Med Chem 65: 11776-11787 (2022)
Novartis Institutes For Biomedical Research
Discovery of a selective c-MET inhibitor with a novel binding mode.
Bioorg Med Chem Lett 75: (2022)
Astrazeneca
Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents.
Bioorg Med Chem 71: (2022)
Sun Yat-Sen University
Modifying a Hydroxyl Patch in Glucagon-like Peptide 1 Produces Biased Agonists with Unique Signaling Profiles.
J Med Chem 65: 11759-11775 (2022)
The University of Queensland
Discovery of (
J Med Chem 65: 11703-11725 (2022)
Jagiellonian University Medical College
Discovery of Insulin/GLP-1/Glucagon Triagonists for the Treatment of Diabetes and Obesity.
ACS Med Chem Lett 13: 1255-1261 (2022)
Merck
Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance.
ACS Med Chem Lett 13: 1286-1294 (2022)
China Pharmaceutical University
Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.
ACS Med Chem Lett 13: 1321-1328 (2022)
Nodthera
Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8
ACS Med Chem Lett 13: 1295-1301 (2022)
Astrazeneca
Novel RXFP1Modulators for Treating Heart Failure.
ACS Med Chem Lett 13: 1213-1214 (2022)
Smith, Gambrell & Russell
Novel IRAK4 Inhibitors for Treating Asthma.
ACS Med Chem Lett 13: 1219-1220 (2022)
Smith, Gambrell & Russell
Discovery of Desmuramylpeptide NOD2 Agonists with Single-Digit Nanomolar Potency.
ACS Med Chem Lett 13: 1270-1277 (2022)
University of Ljubljana
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy.
ACS Med Chem Lett 13: 1217-1218 (2022)
Smith, Gambrell & Russell
Novel Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough.
ACS Med Chem Lett 13: 1215-1216 (2022)
Smith, Gambrell & Russell
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes.
ACS Med Chem Lett 13: 1248-1254 (2022)
Merck
Small-Molecule Inhibitors of the MLL1 CXXC Domain, an Epigenetic Reader of DNA Methylation.
ACS Med Chem Lett 13: 1363-1369 (2022)
University of Virginia
Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.
ACS Med Chem Lett 13: 1351-1357 (2022)
Mitsubishi Tanabe Pharma
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A
J Med Chem 65: 11648-11657 (2022)
University of Southern California
Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[
J Med Chem 65: 11876-11888 (2022)
Guangzhou University of Chinese Medicine
Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease.
Bioorg Med Chem Lett 74: (2022)
Pharmaxis
Novel N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides exhibit selective cytotoxic activity at nanomolar doses towards human leukemic T-cells.
Eur J Med Chem 241: (2022)
Ivan Franko National University of Lviv
Structure activity relationships leading to the identification of the indirect activator of AMPK, R419.
Bioorg Med Chem 71: (2022)
Rigel Pharmaceuticals
Beyond Retigabine: Design, Synthesis, and Pharmacological Characterization of a Potent and Chemically Stable Neuronal Kv7 Channel Activator with Anticonvulsant Activity.
J Med Chem 65: 11340-11364 (2022)
University of Salerno
Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections.
J Med Chem 65: 11388-11403 (2022)
Bristol Myers Squibb
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir.
ACS Med Chem Lett 13: 1345-1350 (2022)
Experimental Drug Development Centre
Identification of Monosaccharide Derivatives as Potent, Selective, and Orally Bioavailable Inhibitors of Human and Mouse Galectin-3.
J Med Chem 65: 11084-11099 (2022)
Bristol Myers Squibb
-Benzyl Benzamide Derivatives as Selective Sub-Nanomolar Butyrylcholinesterase Inhibitors for Possible Treatment in Advanced Alzheimer's Disease.
J Med Chem 65: 11365-11387 (2022)
China Pharmaceutical University
Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases: Discovery of ACT-672125.
J Med Chem 65: 11533-11549 (2022)
Idorsia Pharmaceuticals
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.
J Med Chem 65: 10709-10754 (2022)
Jadavpur University
Recent advances in combretastatin A-4 codrugs for cancer therapy.
Eur J Med Chem 241: (2022)
Xinxiang Medical University
An overview on Estrogen receptors signaling and its ligands in breast cancer.
Eur J Med Chem 241: (2022)
Zhejiang University
New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity.
Eur J Med Chem 241: (2022)
Mansoura University
Structure-Activity relationship study of benzothiophene oxobutanoic acid analogues leading to novel stimulator of interferon gene (STING) agonists.
Eur J Med Chem 241: (2022)
Shanghai Jiao Tong University
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Bioorg Med Chem Lett 74: (2022)
Deciphera Pharmaceuticals
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).
Bioorg Med Chem Lett 74: (2022)
Deciphera Pharmaceuticals
Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance.
Eur J Med Chem 241: (2022)
Central China Normal University
Design and synthesis of novel benzimidazole derivatives as potential Pseudomonas aeruginosa anti-biofilm agents inhibiting LasR: Evidence from comprehensive molecular dynamics simulation and in vitro investigation.
Eur J Med Chem 241: (2022)
Modern University For Technology and Information Mti
Discovery of MDM2-p53 and MDM4-p53 protein-protein interactions small molecule dual inhibitors.
Eur J Med Chem 241: (2022)
Universidade De Lisboa
Benzylaminofentanyl derivates: Discovery of bifunctional μ opioid and σ
Eur J Med Chem 241: (2022)
Jiangsu Ocean University
Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand.
J Med Chem 65: 10992-11009 (2022)
Shanghai Institute of Traumatology and Orthopaedics
Construction of Covalent Bisubstrate Inhibitor of Protein Kinase Reacting with Cysteine Residue at Substrate-Binding Site.
J Med Chem 65: 10975-10991 (2022)
University of Tartu
Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits.
J Med Chem 65: 11607-11632 (2022)
Csir-Indian Institute of Chemical Biology
4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity.
Eur J Med Chem 241: (2022)
Xihua University
Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis.
J Med Chem 65: 14348-14365 (2022)
China Pharmaceutical University
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
J Med Chem 65: 11150-11176 (2022)
Biocon-Bristol Myers Squibb Research and Development Centre
Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA
J Med Chem 65: 10956-10974 (2022)
Universidad Complutense De Madrid
Nostosin G and Spiroidesin B from the Cyanobacterium
J Nat Prod 85: 2000-2005 (2022)
TBA
Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists.
J Med Chem 65: 11270-11290 (2022)
University of Glasgow
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.
J Med Chem 65: 10898-10919 (2022)
Oregon Health and Science University
Development and profiling of mGlu
Bioorg Med Chem Lett 74: (2022)
Vanderbilt University
Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis.
Bioorg Med Chem Lett 74: (2022)
Merck
S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation.
Bioorg Med Chem 71: (2022)
Zhejiang Chinese Medical University
Crescent-shaped meta-substituted benzene derivatives as a new class of non-nucleoside ribonuclease A inhibitors.
Bioorg Med Chem 71: (2022)
Indian Institute of Technology Kharagpur
Updated chemical scaffolds of ABCG2 inhibitors and their structure-inhibition relationships for future development.
Eur J Med Chem 241: (2022)
Dr. Harisingh Gour University
Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
Eur J Med Chem 241: (2022)
Qilu University of Technology (Shandong Academy of Sciences)
Design, synthesis and antitumor evaluation of ATP dual-mimic 2,4-diarylaminopyrimidine and aminoindazole conjugates as potent anaplastic lymphoma kinase inhibitors.
Eur J Med Chem 241: (2022)
Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
Eur J Med Chem 241: (2022)
Peking Union Medical College and Chinese Academy of Medical Sciences
Recent research and development of inhibitors targeting sentrin-specific protease 1 for the treatment of cancers.
Eur J Med Chem 241: (2022)
Sichuan University
Rational Design and Optimization of m
J Med Chem 65: 10920-10937 (2022)
University of California San Diego
Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors
J Med Chem 65: 11550-11573 (2022)
Shandong University
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
J Med Chem 65: 10755-10808 (2022)
Beijing Normal University
Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor.
J Med Chem 65: 10882-10897 (2022)
Mitsubishi Tanabe Pharma
Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13.
J Med Chem 65: 11066-11083 (2022)
Jinan University
Discovery of 1-(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity.
J Med Chem 65: 11214-11228 (2022)
Nanjing Medical University
Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis.
Bioorg Med Chem 71: (2022)
Universit£
High ligand efficiency quinazoline compounds as novel A
Eur J Med Chem 241: (2022)
Univ. Lille
Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
Eur J Med Chem 241: (2022)
Universit£
Identification of 2-hydroxybenzoic acid derivatives as selective SIRT5 inhibitors.
Eur J Med Chem 241: (2022)
University of Michigan
In vitro and in vivo neuroprotective effect of novel mPGES-1 inhibitor in animal model of Parkinson's disease.
Bioorg Med Chem Lett 74: (2022)
Kyung Hee University
Multivalent glucosidase inhibitors based on perylene bisimide and iminosugar conjugates.
Eur J Med Chem 241: (2022)
Hebei University
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
Eur J Med Chem 241: (2022)
Anhui University of Chinese Medicine
Synthesis and biological evaluation of 4-hydroxy-methylpiperidinyl-N-benzyl-acylarylhydrazone hybrids designed as novel multifunctional drug candidates for Alzheimer's disease.
Bioorg Med Chem 71: (2022)
Federal University of Alfenas
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
J Med Chem 65: 11177-11186 (2022)
Constellation, A Morphosys
Unveiling the Structure-Activity Relationships at the Orthosteric Binding Site of P2X Ion Channels: The Route to Selectivity.
J Med Chem 65: 11291-11308 (2022)
European Institute For Molecular Imaging (Eimi)
Pyrrospirones K-Q, Decahydrofluorene-Class Alkaloids from the Marine-Derived Fungus
J Nat Prod 85: 2071-2081 (2022)
Chinese Academy of Sciences
Design and Validation of the First Family of Photo-Activatable Ligands for Melatonin Receptors.
J Med Chem 65: 11229-11240 (2022)
Universit£
Novel Macrocyclic Urea Orexin Receptor Agonists for Treating Sleep Disorders.
ACS Med Chem Lett 13: 1010-1011 (2022)
Smith, Gambrell & Russell
SARS-CoV-2: Novel Therapeutic Approaches for Diagnosis and Treatment.
ACS Med Chem Lett 13: 999-1001 (2022)
Usona Institute
Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough.
ACS Med Chem Lett 13: 1002-1003 (2022)
Smith, Gambrell & Russell
Novel MRGX2 Antagonists for Treating Diseases.
ACS Med Chem Lett 13: 1006-1007 (2022)
Smith, Gambrell & Russell
Benzimidazolone Derivatives as DGAT2 Inhibitors for Treating Diseases.
ACS Med Chem Lett 13: 1004-1005 (2022)
Smith, Gambrell & Russell
Novel N-Linked Isoquinoline Amides as LRRK2 Inhibitors for Treating Parkinson's Disease.
ACS Med Chem Lett 13: 1008-1009 (2022)
Smith, Gambrell & Russell
Synthesis and human monoamine oxidase inhibitory activity of novel C2-, C3- and C4-substituted phthalonitriles.
Bioorg Med Chem Lett 74: (2022)
University of Khartoum
Discovery and Mechanistic Study of
J Med Chem 65: 11058-11065 (2022)
Sichuan University
Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity.
Bioorg Med Chem 71: (2022)
Astellas Pharma
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
Bioorg Med Chem 71: (2022)
Mirati Therapeutics
Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HT
Bioorg Med Chem 71: (2022)
Hec Research and Development Center
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
J Med Chem 65: 11187-11213 (2022)
China Pharmaceutical University
-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
J Med Chem 65: 11241-11256 (2022)
Janssen Research and Development
Sodium-Glucose Cotransporter Inhibitors as Antidiabetic Drugs: Current Development and Future Perspectives.
J Med Chem 65: 10848-10881 (2022)
University of Messina
Design, synthesis and biological evaluation of light-driven on-off multitarget AChE and MAO-B inhibitors.
RSC Med Chem 13: 873-883 (2022)
Universit�
Development of subtype-selective covalent ligands for the adenosine A
RSC Med Chem 13: 850-856 (2022)
Leiden University
FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms.
RSC Med Chem 13: 798-816 (2022)
University of Arkansas
Discovery of Novel 7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-
J Med Chem 65: 11257-11269 (2022)
Tongji University
Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.
J Med Chem 65: 11126-11149 (2022)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)
Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity.
RSC Med Chem 13: 817-821 (2022)
University of Cambridge
design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region.
RSC Med Chem 13: 831-839 (2022)
University of Leeds
DNA-encoded library screening on two validated enzymes of the peptidoglycan biosynthetic pathway.
Bioorg Med Chem Lett 73: (2022)
University of Ljubljana
Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line.
Bioorg Med Chem Lett 73: (2022)
Universit£
Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents.
Bioorg Med Chem 71: (2022)
Zhejiang University
Development of potent non-acylhydrazone inhibitors of intestinal sodium-dependent phosphate transport protein 2b (NaPi2b).
Bioorg Med Chem 71: (2022)
Hokkaido University
Nucleic-Acid-Based Targeted Degradation in Drug Discovery.
J Med Chem 65: 10217-10232 (2022)
Second Military Medical University
Design, Synthesis, and Biological Evaluation of Pyrrole-2-carboxamide Derivatives as Mycobacterial Membrane Protein Large 3 Inhibitors for Treating Drug-Resistant Tuberculosis.
J Med Chem 65: 10534-10553 (2022)
Peking Union Medical College and Chinese Academy of Medical Sciences
Synthesis and activity evaluation of selenazole-coupled CPI-1 irreversible bifunctional inhibitors for botulinum toxin A light chain.
Bioorg Med Chem Lett 73: (2022)
Guizhou Medical University
Protein Lysine Methyltransferase SMYD2: A Promising Small Molecule Target for Cancer Therapy.
J Med Chem 65: 10119-10132 (2022)
Zhejiang University
Optimization of Covalent MKK7 Inhibitors
J Med Chem 65: 10341-10356 (2022)
Weizmann Institute of Science
Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking.
Bioorg Med Chem Lett 73: (2022)
Siberian Branch of The Russian Academy of Science
Discovery of 2-vinyl-10H-phenothiazine derivatives as a class of ferroptosis inhibitors with minimal human Ether-a-go-go related gene (hERG) activity for the treatment of DOX-induced cardiomyopathy.
Bioorg Med Chem Lett 74: (2022)
Sichuan University
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
J Med Chem 65: 10655-10673 (2022)
Shionogi
Anti-inflammatory and anticancer p-terphenyl derivatives from fungi of the genus Thelephora.
Bioorg Med Chem 70: (2022)
Oncowitan
Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β
J Med Chem 65: 10233-10250 (2022)
Chiesi Farmaceutici
Is a Highly Selective and Potent κ Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity.
J Med Chem 65: 10377-10392 (2022)
Fudan University
DEAD-Box Helicase DDX3X as a Host Target against Emerging Viruses: New Insights for Medicinal Chemical Approaches.
J Med Chem 65: 10195-10216 (2022)
University of Siena
Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos.
J Med Chem 65: 10611-10625 (2022)
Icahn School of Medicine At Mount Sinai
Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors.
J Med Chem 65: 10408-10418 (2022)
Jinan University
Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
J Med Chem 65: 10251-10284 (2022)
Repare Therapeutics
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.
J Med Chem 65: 10133-10160 (2022)
West China Hospital
Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α.
J Med Chem 65: 10318-10340 (2022)
Merck
General Pharmacological Activation Mechanism of K
J Med Chem 65: 10285-10299 (2022)
East China Normal University
Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Eur J Med Chem 241: (2022)
Dalian Medical University
Identification and structural analysis of a selective tropomyosin receptor kinase C (TRKC) inhibitor.
Eur J Med Chem 241: (2022)
China Pharmaceutical University
Exploring the roles of the Cdc2-like kinases in cancers.
Bioorg Med Chem 70: (2022)
University of Canterbury
Synthesis and evaluation of hydrazinyl-containing pyrrolo[2,3-d]pyrimidine series as potent, selective and oral JAK1 inhibitors for the treatment of rheumatoid arthritis.
Bioorg Med Chem Lett 74: (2022)
Wuxi Apptec (Shanghai) Co.
Discovery of two novel (4-hydroxyphenyl) substituted polycyclic carbocycles as potent and selective estrogen receptor beta agonists.
Bioorg Med Chem Lett 73: (2022)
Marquette University
New naphtho/thienobenzo-triazoles with interconnected anti-inflammatory and cholinesterase inhibitory activity.
Eur J Med Chem 241: (2022)
University of Zagreb
Discovery and antiviral profile of new sulfamoylbenzamide derivatives as HBV capsid assembly modulators.
Bioorg Med Chem Lett 73: (2022)
Promidis
Discovery of novel human lactate dehydrogenase inhibitors: Structure-based virtual screening studies and biological assessment.
Eur J Med Chem 240: (2022)
Sapienza University of Rome
Scaffold modified Vemurafenib analogues as highly selective mitogen activated protein kinase kinase 4 (MKK4) inhibitors.
Eur J Med Chem 240: (2022)
Eberhard Karls Universit£T T£Bingen
Current progress and novel strategies that target CDK12 for drug discovery.
Eur J Med Chem 240: (2022)
West China Hospital
-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression.
J Med Chem 65: 10481-10505 (2022)
Lanzhou University
Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity.
J Med Chem 65: 10441-10458 (2022)
University of Minnesota
Bicyclic pyrimidine compounds as potent IRAK4 inhibitors.
Bioorg Med Chem Lett 73: (2022)
Rigel Pharmaceuticals
Discovery of potent benzoxaborole inhibitors against SARS-CoV-2 main and dengue virus proteases.
Eur J Med Chem 240: (2022)
Heidelberg University
The untapped potential of spermidine alkaloids: Sources, structures, bioactivities and syntheses.
Eur J Med Chem 240: (2022)
Beijing University of Chinese Medicine
A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing.
Bioorg Med Chem 70: (2022)
China Pharmaceutical University
Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia.
Bioorg Med Chem 70: (2022)
Nanjing University of Chinese Medicine
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
J Med Chem 65: 10419-10440 (2022)
Janssen Research & Development
Discovery of Hexahydrofuro[3,2-
J Med Chem 65: 10674-10690 (2022)
Jinan University
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
ACS Med Chem Lett 13: 1159-1164 (2022)
Incyte
Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells.
ACS Med Chem Lett 13: 1062-1067 (2022)
Goethe University Frankfurt
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
ACS Med Chem Lett 13: 1165-1171 (2022)
Bristol Myers Squibb
Spiro-naphthyridine Antagonists of the Melanocortin Receptor 4 for the Treatment of Cachexia Associated with Chronic Illness.
ACS Med Chem Lett 13: 997-998 (2022)
Arrival Discovery
Discovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na
ACS Med Chem Lett 13: 1043-1051 (2022)
Ardelyx
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.
ACS Med Chem Lett 13: 1131-1136 (2022)
Chonnam National University
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
ACS Med Chem Lett 13: 1172-1181 (2022)
University of Dundee
Development of Urea-Bond-Containing Michael Acceptors as Antitrypanosomal Agents Targeting Rhodesain.
ACS Med Chem Lett 13: 1083-1090 (2022)
University of Messina
Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B.
ACS Med Chem Lett 13: 1091-1098 (2022)
J. Michael Bishop Institute of Cancer Research
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies.
ACS Med Chem Lett 13: 1137-1143 (2022)
Epizyme
Discovery of Benzylpiperazine Derivatives as CNS-Penetrant and Selective Histone Deacetylase 6 Inhibitors.
ACS Med Chem Lett 13: 1077-1082 (2022)
Kansai University
Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
ACS Med Chem Lett 13: 1099-1108 (2022)
Ucb
Inhibitor Screen Identifies Covalent Inhibitors of the Protein Histidine Phosphatase PHPT1.
ACS Med Chem Lett 13: 1198-1201 (2022)
University of Utah College of Pharmacy
A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-
ACS Med Chem Lett 13: 1151-1158 (2022)
University of North Carolina
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
Eur J Med Chem 240: (2022)
Lanzhou University
Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
Eur J Med Chem 240: (2022)
Taipei Medical University
Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
Eur J Med Chem 240: (2022)
Ludwig-Maximilians University
Discovery of pyridyl urea sulfonamide inhibitors of Na
Bioorg Med Chem Lett 73: (2022)
Moma Therapeutics
Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. An update from 2017 to early 2022.
Eur J Med Chem 240: (2022)
Universit£
AI-based prediction of new binding site and virtual screening for the discovery of novel P2X3 receptor antagonists.
Eur J Med Chem 240: (2022)
Gwangju Institute of Science and Technology
The overview of Mitogen-activated extracellular signal-regulated kinase (MEK)-based dual inhibitor in the treatment of cancers.
Bioorg Med Chem 70: (2022)
Zhengzhou University
Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands.
J Med Chem 65: 9918-9938 (2022)
University of Pisa
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
J Med Chem 65: 9750-9788 (2022)
Johannes Gutenberg University Mainz
Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors.
Bioorg Med Chem Lett 73: (2022)
Institut Pasteur Korea
Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis.
Bioorg Med Chem Lett 73: (2022)
Nimbus Therapeutics
Targeting the interaction of β-catenin and TCF/LEF transcription factors to inhibit oncogenic Wnt signaling.
Bioorg Med Chem 70: (2022)
Vu University Amsterdam
Sortase A-mediated cyclization of novel polycyclic RGD peptides for α
Bioorg Med Chem Lett 73: (2022)
Hefei Normal University
A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.
Eur J Med Chem 240: (2022)
Texas A&M University
Discovery of novel orexin receptor antagonists using a 1,3,5-trioxazatriquinane bearing multiple effective residues (TriMER) library.
Eur J Med Chem 240: (2022)
University of Tsukuba
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT
Bioorg Med Chem 70: (2022)
Hec Pharm Group
Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer.
J Med Chem 65: 9662-9677 (2022)
Blueprint Medicines
Recent Advances with KDM4 Inhibitors and Potential Applications.
J Med Chem 65: 9564-9579 (2022)
St. Jude Children'S Research Hospital
Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.
Bioorg Med Chem Lett 73: (2022)
Incyte Research Institute
4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors.
Eur J Med Chem 240: (2022)
Cardiff University
Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
Eur J Med Chem 240: (2022)
Keimyung University
From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
J Med Chem 65: 10079-10097 (2022)
Universit£
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.
J Med Chem 65: 9873-9892 (2022)
China Pharmaceutical University
Semisynthesis of Hypothemycin Analogues Targeting the C8-C9 Diol.
J Nat Prod 85: 2018-2025 (2022)
University of North Carolina At Greensboro
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
J Med Chem 65: 9678-9690 (2022)
Mirati Therapeutics
Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on α-Hydroxy-β-amino Acid Derivatives of Bestatin.
J Med Chem 65: 10098-10117 (2022)
National Centre For Scientific Research "Demokritos
Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.
J Med Chem 65: 9893-9917 (2022)
West China Hospital
Identification of Human Alanine-Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1.
J Med Chem 65: 9718-9734 (2022)
University of Perugia
The discovery of a non-competitive GOT1 inhibitor, hydralazine hydrochloride, via a coupling reaction-based high-throughput screening assay.
Bioorg Med Chem Lett 73: (2022)
Nanjing University of Chinese Medicine
A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.
Eur J Med Chem 240: (2022)
Zhengzhou University
Discovery and Optimization of a Synthetic Class of Nectin-4-Targeted CD137 Agonists for Immuno-oncology.
J Med Chem 65: 9858-9872 (2022)
Bicycle Therapeutics
Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Bioorg Med Chem Lett 73: (2022)
Bristol-Myers Squibb Research & Early Development
Seeking heterocyclic scaffolds as antivirals against dengue virus.
Eur J Med Chem 240: (2022)
National Institute of Technology
Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease.
J Med Chem 65: 9819-9845 (2022)
Charles River Laboratories
CDK9 inhibitors in cancer research.
RSC Med Chem 13: 688-710 (2022)
Nankai University
Encoding BRAF inhibitor functions in protein degraders.
RSC Med Chem 13: 731-736 (2022)
The Institute of Cancer Research
Inhibition of MARK4 by serotonin as an attractive therapeutic approach to combat Alzheimer's disease and neuroinflammation.
RSC Med Chem 13: 737-745 (2022)
Jamia Millia Islamia
Design, synthesis and antitumor activity study of a gemcitabine prodrug conjugated with a HDAC6 inhibitor.
Bioorg Med Chem Lett 72: (2022)
Qingdao University Medical College
Novel anilinopyrimidine derivatives as potential EGFR
Bioorg Med Chem 70: (2022)
Southeast University
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
Bioorg Med Chem Lett 72: (2022)
H. Lundbeck
Synthesis and biological evaluation of novel pentanediamide derivatives as S-adenosyl-l-homocysteine hydrolase inhibitors.
Bioorg Med Chem Lett 72: (2022)
Guilin Medical University
Therapeutic Potential and Activity Modulation of the Protein Lysine Deacylase Sirtuin 5.
J Med Chem 65: 9580-9606 (2022)
Sapienza University of Rome
Design, Synthesis, and Characterization of [
J Med Chem 65: 9939-9954 (2022)
Harvard Medical School
Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
Eur J Med Chem 240: (2022)
Universit£
Chalcone-amide, a privileged backbone for the design and development of selective SARS-CoV/SARS-CoV-2 papain-like protease inhibitors.
Eur J Med Chem 240: (2022)
Mazandaran University of Medical Sciences
Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability.
Eur J Med Chem 240: (2022)
Yanbian University College of Pharmacy
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
Eur J Med Chem 240: (2022)
Mcgill University
Medicinal Chemistry and Chemical Biology of Nurr1 Modulators: An Emerging Strategy in Neurodegeneration.
J Med Chem 65: 9548-9563 (2022)
Goethe University Frankfurt
Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors.
J Med Chem 65: 9531-9547 (2022)
China Pharmaceutical University
7-Azaindole, 2,7-diazaindole, and 1H-pyrazole as core structures for novel anticancer agents with potential chemosensitizing properties.
Eur J Med Chem 240: (2022)
University Hospital Hradec Kralove
Structure-Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors.
J Med Chem 65: 10638-10654 (2022)
Chinese Academy of Sciences
The protective effects of natural product tunicatachalcone against neuroinflammation via targeting RIPK2 in microglia BV-2 cells stimulated by LPS.
Bioorg Med Chem 69: (2022)
Hebei Medical University
Design, Synthesis, and Structure-Activity Relationship Studies of Bisamide Derivatives of Amphotericin B with Potent Efficacy and Low Toxicity.
J Med Chem 65: 8897-8913 (2022)
Shanghai Institute of Materia Medica
Glioblastoma: Current Status, Emerging Targets, and Recent Advances.
J Med Chem 65: 8596-8685 (2022)
Taipei Medical University
Discovery of Potent Small-Molecule USP8 Inhibitors for the Treatment of Breast Cancer through Regulating ERα Expression.
J Med Chem 65: 8914-8932 (2022)
China Pharmaceutical University
-Acylamino Saccharin as an Emerging Cysteine-Directed Covalent Warhead and Its Application in the Identification of Novel FBPase Inhibitors toward Glucose Reduction.
J Med Chem 65: 9126-9143 (2022)
Central China Normal University
Therapeutic Strategies to Target the Androgen Receptor.
J Med Chem 65: 8772-8797 (2022)
University of Michigan
Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone.
Eur J Med Chem 240: (2022)
Shanghai Jiao Tong University
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.
Bioorg Med Chem 69: (2022)
West China Hospital of Sichuan University
Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.
Eur J Med Chem 240: (2022)
Shandong University
Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 72: (2022)
Hebei University
Design, synthesis, and bioactivity evaluation of macrocyclic benzo[b]pyrido[4,3-e][1,4]oxazine derivatives as novel Pim-1 kinase inhibitors.
Bioorg Med Chem Lett 72: (2022)
Beijing University of Chemical Technology
A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.
Eur J Med Chem 240: (2022)
Texas A&M University
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
Bioorg Med Chem Lett 72: (2022)
Wuxi Apptec
Synthesis and evaluation of inhibitors of Mycobacterium tuberculosis UGM using bioisosteric replacement.
Bioorg Med Chem 69: (2022)
Guizhou University of Traditional Chinese Medicine
Improving the solubility and antileukemia activity of Wnt/β-catenin signaling inhibitors by disrupting molecular planarity.
Bioorg Med Chem 69: (2022)
University of Maryland
Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy.
Eur J Med Chem 240: (2022)
Lanzhou University
Small Carbohydrate Derivatives as Potent Antibiofilm Agents.
J Med Chem 65: 8525-8549 (2022)
Indian Institute of Technology Bombay
Structure-activity relationships of 2-pyrimidinecarbohydrazides as utrophin modulators for the potential treatment of Duchenne muscular dystrophy.
Bioorg Med Chem 69: (2022)
University of Oxford
2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors.
Bioorg Med Chem 69: (2022)
Northwestern University
Structure-Based Design, Optimization, and Development of [
J Med Chem 65: 9034-9049 (2022)
Helmholtz-Zentrum Dresden-Rossendorf (Hzdr)
Innovative Non-PrP-Targeted Drug Strategy Designed to Enhance Prion Clearance.
J Med Chem 65: 8998-9010 (2022)
Scuola Internazionale Superiore Di Studi Avanzati (Sissa)
Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response.
J Med Chem 65: 9230-9252 (2022)
The Scripps Research Institute
Discovery of an Oral, Rule of 5 Compliant, Interleukin 17A Protein-Protein Interaction Modulator for the Potential Treatment of Psoriasis and Other Inflammatory Diseases.
J Med Chem 65: 8828-8842 (2022)
Leo Pharma Research & Early Development
: A Prolific Source of Bioactive Secondary Metabolites with Therapeutic Potential.
J Med Chem 65: 8735-8771 (2022)
Zhejiang University
Design, synthesis, and bioactivity study on Lissodendrins B derivatives as PARP1 inhibitor.
Bioorg Med Chem 69: (2022)
Ocean University of China
Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors.
Bioorg Med Chem 69: (2022)
University of Sharjah
Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.
J Med Chem 65: 10506-10522 (2022)
Icahn School of Medicine At Mount Sinai
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead
J Med Chem 65: 9206-9229 (2022)
Merck Healthcare
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.
J Med Chem 65: 8798-8827 (2022)
Second Military Medical University
Orally Bioavailable Enzymatic Inhibitor of CD38,
J Med Chem 65: 9418-9446 (2022)
Mitobridge (An Astellas)
Discovery of 2-thiobenzimidazoles as noncovalent inhibitors of SARS-CoV-2 main protease.
Bioorg Med Chem Lett 72: (2022)
New York University Abu Dhabi
Near-Infrared Fluorescent Probes as Imaging and Theranostic Modalities for Amyloid-Beta and Tau Aggregates in Alzheimer's Disease.
J Med Chem 65: 8550-8595 (2022)
Indian Institute of Technology (Bhu)
Small-Molecule Gankyrin Inhibition as a Therapeutic Strategy for Breast and Lung Cancer.
J Med Chem 65: 8975-8997 (2022)
St. John'S University
Discovery of potent dual ligands for dopamine D4 and σ1 receptors.
Bioorg Med Chem 69: (2022)
Bioprojet-Biotech
Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ.
Bioorg Med Chem 69: (2022)
La Trobe University
Recent advances on synthesis and biological activities of C-17 aza-heterocycle derived steroids.
Bioorg Med Chem 69: (2022)
Changzhi University
Novel Hybrids of 3-Substituted Coumarin and Phenylsulfonylfuroxan as Potent Antitumor Agents with Collateral Sensitivity against MCF-7/ADR.
J Med Chem 65: 9328-9349 (2022)
Fudan University
Cosolvent Sites-Based Discovery of
J Med Chem 65: 9691-9705 (2022)
Universidad De Buenos Aires
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H
J Med Chem 65: 8258-8288 (2022)
University of Nottingham Biodiscovery Institute
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir.
J Med Chem 65: 8686-8698 (2022)
Texas A&M University
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
J Med Chem 65: 8843-8854 (2022)
Bristol-Myers Squibb Research & Early Development
Examining the Role of the Linker in Bitopic
J Med Chem 65: 9076-9095 (2022)
Monash University
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.
J Med Chem 65: 9350-9375 (2022)
Weill Cornell Medicine
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
Bioorg Med Chem Lett 72: (2022)
University of Trieste
Identification and in vitro characterization of a new series of potent and highly selective G9a inhibitors as novel anti-fibroadipogenic agents.
Bioorg Med Chem Lett 72: (2022)
Promidis
Indoloquinolines as scaffolds for the design of potent G-quadruplex ligands.
Bioorg Med Chem Lett 72: (2022)
Universidade De Lisboa
Defined stereoisomers of 2″-amino NAD
Bioorg Med Chem 68: (2022)
King'S College London
Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
Bioorg Med Chem 68: (2022)
Eindhoven University of Technology
Discovery of Novel Benzo[4,5]imidazo[1,2-
J Med Chem 65: 8933-8947 (2022)
Sun Yat-Sen University
Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.
J Med Chem 65: 9376-9395 (2022)
Eberhard Karls University T£Bingen
Structure-Guided Optimization of Small-Molecule Folate Uptake Inhibitors Targeting the Energy-Coupling Factor Transporters.
J Med Chem 65: 8869-8880 (2022)
Institute For Pharmaceutical Research Saarland (Hips)
Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).
J Med Chem 65: 9312-9327 (2022)
West China Hospital
Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology.
J Med Chem 65: 8961-8974 (2022)
Merck
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
ACS Med Chem Lett 13: 955-963 (2022)
The Ohio State University
Modified Benzofuran-carboxamide Compounds as Glucosylceramide Synthase Inhibitors for Treating Diseases.
ACS Med Chem Lett 13: 879-880 (2022)
Smith, Gambrell & Russell
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
ACS Med Chem Lett 13: 943-948 (2022)
Bristol Myers Squibb Research and Development
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy.
ACS Med Chem Lett 13: 883-884 (2022)
Smith, Gambrell & Russell
Ibogaine and Their Analogs as Therapeutics for Neurological and Psychiatric Disorders.
ACS Med Chem Lett 13: 888-890 (2022)
Usona Institute
Drug-like Inhibitors of DC-SIGN Based on a Quinolone Scaffold.
ACS Med Chem Lett 13: 935-942 (2022)
Max Planck Institute of Colloids and Interfaces
Novel 6-Methoxy-3,4-dihydro-1
ACS Med Chem Lett 13: 891-892 (2022)
Smith, Gambrell & Russell
Diazepinone Compounds as Sppl2a Inhibitors for Treating Autoimmune Diseases and Lymphomas.
ACS Med Chem Lett 13: 881-882 (2022)
Smith, Gambrell & Russell
Application of Rapidly Accelerating Fibrosarcoma Protein Degraders in Drug Discovery.
ACS Med Chem Lett 13: 885-887 (2022)
Usona Institute
Discovery of a High Affinity Adenosine A
ACS Med Chem Lett 13: 923-934 (2022)
University of Cambridge
Novel Bis-phosphoglycerate Mutase Modulators for Treating Sickle Cell Disease.
ACS Med Chem Lett 13: 877-878 (2022)
Smith, Gambrell & Russell
Novel Halomethylketone Azadipeptides for Treating COVID-19.
ACS Med Chem Lett 13: 875-876 (2022)
A*Star
Targeting NOX2 via p47/phox-p22/phox Inhibition with Novel Triproline Mimetics.
ACS Med Chem Lett 13: 949-954 (2022)
Universit£
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.
J Med Chem 65: 9459-9477 (2022)
Chinese Academy of Sciences
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
J Med Chem 65: 8948-8960 (2022)
Biocon-Bristol Myers Squibb Research and Development Center
Design and synthesis of a novel non peptide CN-NFATc signaling inhibitor for tumor suppression in triple negative breast cancer.
Eur J Med Chem 238: (2022)
Universitat Aut£Noma De Barcelona
Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
Bioorg Med Chem Lett 72: (2022)
Shenyang Pharmaceutical University
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
Eur J Med Chem 238: (2022)
Universit£
Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
Eur J Med Chem 238: (2022)
College of Pharmacy of Liaoning University
Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy.
Eur J Med Chem 238: (2022)
National Clinical Research Center For Geriatrics
Synthesis and application of phosphorylated saccharides in researching carbohydrate-based drugs.
Bioorg Med Chem 68: (2022)
Henan University of Chinese Medicine
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.
J Med Chem 65: 8303-8331 (2022)
University of Kansas
Hematopoietic Progenitor Kinase 1 in Tumor Immunology: A Medicinal Chemistry Perspective.
J Med Chem 65: 8065-8090 (2022)
China Pharmaceutical University
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.
J Med Chem 65: 11010-11033 (2022)
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of new thalidomide-donepezil hybrids as neuroprotective agents targeting cholinesterases and neuroinflammation.
RSC Med Chem 13: 568-584 (2022)
Federal University of Alfenas
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs.
RSC Med Chem 13: 522-567 (2022)
Mansoura University
Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.
RSC Med Chem 13: 497-510 (2022)
University of Otago Dunedin
Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances.
Eur J Med Chem 238: (2022)
Shandong University
Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants.
Eur J Med Chem 238: (2022)
Shenyang Pharmaceutical University
Entry inhibition of hepatitis B virus using cyclosporin O derivatives with peptoid side chain incorporation.
Bioorg Med Chem 68: (2022)
Gwangju Insitute of Science and Technology (Gist)
Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease.
Eur J Med Chem 238: (2022)
Southern Medical University
Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.
Bioorg Med Chem Lett 72: (2022)
Abbvie
Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.
Eur J Med Chem 238: (2022)
Peking University
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
Eur J Med Chem 238: (2022)
University of Hradec Kralove
Discovery of Aryloxyphenyl-Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis.
J Med Chem 65: 8493-8510 (2022)
Taisho Pharmaceutical
Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides.
J Med Chem 65: 8289-8302 (2022)
Ningxia Medical University
Identification and Characterization of Natural and Semisynthetic Quinones as Aurora Kinase Inhibitors.
J Nat Prod 85: 1503-1513 (2022)
Lahore University of Management Sciences
Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity.
J Med Chem 65: 8456-8477 (2022)
Takeda Pharmaceutical
Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors.
RSC Med Chem 13: 471-496 (2022)
Leibniz Institute For Plasma Science and Technology (Inp Greifswald)
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
Eur J Med Chem 238: (2022)
Sichuan University
Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
J Med Chem 65: 8144-8168 (2022)
Nanjing Chia-Tai Tianqing Pharmaceutical
trans, trans-2-C-Aryl-3,4-dihydroxypyrrolidines as potent and selective β-glucosidase inhibitors: Pharmacological chaperones for Gaucher disease.
Eur J Med Chem 238: (2022)
Chinese Academy of Sciences
Tetrahydropyridin-4-ylpicolinoylglycines as novel and orally active prolyl hydroxylase 2 (PHD2) inhibitors for the treatment of renal anemia.
Eur J Med Chem 238: (2022)
China Pharmaceutical University
Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1.
J Med Chem 65: 9011-9033 (2022)
Heidelberg Institute For Theoretical Studies (Hits)
Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.
J Med Chem 65: 8416-8443 (2022)
Icahn School of Medicine At Mount Sinai
Development of an automated screen for Kv7.2 potassium channels and discovery of a new agonist chemotype.
Bioorg Med Chem Lett 71: (2022)
University of Michigan
Early potential evaluation of lead compounds from a DNA-encoded library by the determination of their thermodynamics through a chromatographic method based on immobilized β
Bioorg Med Chem 68: (2022)
Northwest University
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
Eur J Med Chem 238: (2022)
China Pharmaceutical University
Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma.
J Med Chem 65: 9096-9125 (2022)
Zhejiang University
Development of flavonoid probes and the binding mode of the target protein and quercetin derivatives.
Bioorg Med Chem 68: (2022)
Gifu University
Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.
J Med Chem 65: 8444-8455 (2022)
Sun Yat-Sen University
Identification of non-ATP-competitive α-carboline inhibitors of the anaplastic lymphoma kinase.
Eur J Med Chem 238: (2022)
University of Milano-Bicocca
Discovery of non-substrate, environmentally sensitive turn-on fluorescent probes for imaging HDAC8 in tumor cells and tissue slices.
Bioorg Med Chem 68: (2022)
Nanjing University of Chinese Medicine
Chemical analysis of amyloid β aggregation inhibitors derived from Geranium thunbergii.
Bioorg Med Chem 68: (2022)
Muroran Institute of Technology
Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
Bioorg Med Chem Lett 71: (2022)
Lomonosov Moscow State University
Miniproteins in medicinal chemistry.
Bioorg Med Chem Lett 71: (2022)
Wroclaw University of Science and Technology
Therapeutic potentials and structure-activity relationship of 1,3-benzodioxole N-carbamothioyl carboxamide derivatives as selective and potent antagonists of P2X4 and P2X7 receptors.
Eur J Med Chem 238: (2022)
Comsats University Islamabad
Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis.
Eur J Med Chem 238: (2022)
Anhui Medical University
Hybrid Diterpenic Meroterpenoids from an Endophytic
J Nat Prod 85: 1486-1494 (2022)
Kunming Medical University
Selectivity through Targeted Protein Degradation (TPD).
J Med Chem 65: 8113-8126 (2022)
Astrazeneca
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
J Med Chem 65: 8169-8190 (2022)
The Institute of Cancer Research
Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation.
Bioorg Med Chem 68: (2022)
Chinese Academy of Sciences
Evaluation of chromane derivatives: Promising privileged scaffolds for lead discovery within Alzheimer's disease.
Bioorg Med Chem 68: (2022)
University of £Vora
Phage Display Selected Cyclic Peptide Inhibitors of Kallikrein-Related Peptidases 5 and 7 and Their
J Med Chem 65: 9735-9749 (2022)
Ecole Polytechnique F�D�Rale De Lausanne (Epfl)
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6
J Med Chem 65: 8191-8207 (2022)
The Institute of Cancer Research
Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
J Med Chem 65: 8380-8400 (2022)
Yale University
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
J Med Chem 65: 8127-8143 (2022)
Mitsubishi Tanabe Pharma
Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer.
Eur J Med Chem 238: (2022)
China Pharmaceutical University
Structure-Based Discovery of Novel NH
J Med Chem 65: 8478-8492 (2022)
Fudan University
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
J Med Chem 65: 8208-8226 (2022)
Pfizer
Structure-activity relationships of hydrophobic alkyl acrylamides as tissue transglutaminase inhibitors.
RSC Med Chem 13: 413-428 (2022)
University of Ottawa
Recent developments in the structural characterisation of the IR and IGF1R: implications for the design of IR-IGF1R hybrid receptor modulators.
RSC Med Chem 13: 360-374 (2022)
University of Leeds
Diazepinone HBV capsid assembly modulators.
Bioorg Med Chem Lett 72: (2022)
Janssen Research and Development
Discovery of 5-methyl-1H-benzo[d]imidazole derivatives as novel P2X3 Receptor antagonists.
Bioorg Med Chem Lett 72: (2022)
Gwangju Institute of Science and Technology (Gist)
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
Bioorg Med Chem Lett 71: (2022)
Chinese Academy of Medical Sciences & Peking Union Medical College
Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
Bioorg Med Chem Lett 71: (2022)
Qingdao University Medical College
Strategies for targeting the P2Y
Bioorg Med Chem Lett 71: (2022)
The University of Sydney
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.
Eur J Med Chem 238: (2022)
Sichuan University
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
Eur J Med Chem 238: (2022)
Shandong University
Glenthmycins A-M: Macrocyclic Spirotetronate Polyketide Antibacterials from the Australian Pasture Plant-Derived
J Nat Prod 85: 1641-1657 (2022)
The University of Queensland
Discovery of Small Molecules Simultaneously Targeting NAD(P)H:Quinone Oxidoreductase 1 and Nicotinamide Phosphoribosyltransferase: Treatment of Drug-Resistant Non-small-Cell Lung Cancer.
J Med Chem 65: 7746-7769 (2022)
China Pharmaceutical University
Scaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy.
J Med Chem 65: 7896-7917 (2022)
East China Normal University
Structure-Guided Design of Potent Spirocyclic Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3C-like Protease.
J Med Chem 65: 7818-7832 (2022)
Wichita State University
Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
Bioorg Med Chem Lett 71: (2022)
Wuxi Apptec
Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
Eur J Med Chem 238: (2022)
Peking University
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Eur J Med Chem 238: (2022)
Guizhou Medical University
Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker.
Eur J Med Chem 238: (2022)
German University In Cairo
Small molecules targeting cGAS-STING pathway for autoimmune disease.
Eur J Med Chem 238: (2022)
Shanghai Jiao Tong University
Selective inhibition of histone deacetylase 3 by novel hydrazide based small molecules as therapeutic intervention for the treatment of cancer.
Eur J Med Chem 238: (2022)
Birla Institute of Technology and Science-Pilani Hyderabad Campus
Development of sulfonamide-based NLRP3 inhibitors: Further modifications and optimization through structure-activity relationship studies.
Eur J Med Chem 238: (2022)
Virginia Commonwealth University
Design, synthesis of DNA-interactive 4-thiazolidinone-based indolo-/pyrroloazepinone conjugates as potential cytotoxic and topoisomerase I inhibitors.
Eur J Med Chem 238: (2022)
National Institute of Pharmaceutical Education and Research (NIPER)
The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate.
Eur J Med Chem 238: (2022)
Nankai University
Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors.
Eur J Med Chem 238: (2022)
Philipps University
Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation.
Bioorg Med Chem 67: (2022)
University of Nebraska Medical Center
Discovery of 1,6-Naphthyridin-2(1
J Med Chem 65: 7595-7618 (2022)
Nanjing University of Chinese Medicine
Design and synthesis of efficient fluororethylene-peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3).
Bioorg Med Chem 67: (2022)
Graz University of Technology
Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.
J Med Chem 65: 7561-7580 (2022)
The State University of New Jersey
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.
Eur J Med Chem 238: (2022)
Shenyang Pharmaceutical University
Organocatalyzed umpolung addition for synthesis of heterocyclic-fused arylidene-imidazolones as anticancer agents.
Bioorg Med Chem 67: (2022)
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery of honokiol thioethers containing 1,3,4-oxadiazole moieties as potential α-glucosidase and SARS-CoV-2 entry inhibitors.
Bioorg Med Chem 67: (2022)
Zhengzhou University
Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL.
J Med Chem 65: 7770-7785 (2022)
China Pharmaceutical University
Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.
J Med Chem 65: 7854-7875 (2022)
Sun Yat-Sen University
Tuberculosis Drug Discovery: Challenges and New Horizons.
J Med Chem 65: 7489-7531 (2022)
University College London
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.
J Med Chem 65: 7993-8010 (2022)
Wuhan University
Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9).
Bioorg Med Chem Lett 75: (2022)
Merck
Discovery of a Novel Series of Imipridone Compounds as
J Med Chem 65: 7629-7655 (2022)
Sichuan University
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
J Med Chem 65: 8011-8028 (2022)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors.
J Med Chem 65: 7656-7681 (2022)
Virginia Tech
Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.
J Med Chem 65: 7532-7560 (2022)
University of Perugia
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-
J Med Chem 65: 7799-7817 (2022)
Goethe University Frankfurt
Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors.
Bioorg Med Chem Lett 70: (2022)
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Bioorg Med Chem Lett 71: (2022)
Crinetics Pharmaceuticals
Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities.
Eur J Med Chem 238: (2022)
Zhengzhou University
Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and selective CDK9 inhibitors that enable transient target engagement for the treatment of hematologic malignancies.
Eur J Med Chem 238: (2022)
China Pharmaceutical University
Glycosylation increases the anti-QS as well as anti-biofilm and anti-adhesion ability of the cyclo (L-Trp-L-Ser) against Pseudomonas aeruginosa.
Eur J Med Chem 238: (2022)
Fujian Normal University
Peptidomimetics: An Overview of Recent Medicinal Chemistry Efforts toward the Discovery of Novel Small Molecule Inhibitors.
J Med Chem 65: 7438-7475 (2022)
Ri.Med Foundation
Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
Bioorg Med Chem Lett 70: (2022)
Shenyang Pharmaceutical University
Development of pyrazolo[3,4-d]pyrimidin-4-one scaffold as novel CDK2 inhibitors: Design, synthesis, and biological evaluation.
Bioorg Med Chem Lett 70: (2022)
Beijing University of Technology
Synthesis and medicinal chemistry of tetronamides: Promising agrochemicals and antitumoral compounds.
Bioorg Med Chem 67: (2022)
Universidade Federal De Minas Gerais
New TRPM8 blockers exert anticancer activity over castration-resistant prostate cancer models.
Eur J Med Chem 238: (2022)
University of Salerno
Design, synthesis and evaluation of inhibitors of the SARS-CoV-2 nsp3 macrodomain.
Bioorg Med Chem 67: (2022)
Mcdaniel College
New peptidomimetic rhodesain inhibitors with improved selectivity towards human cathepsins.
Eur J Med Chem 238: (2022)
Johannes Gutenberg University
Emerging impact of triazoles as anti-tubercular agent.
Eur J Med Chem 238: (2022)
Barauni (A Constituent Unit of Lalit Narayan Mithila University)
Discovery of a potent, selective and cell active inhibitor of m
Eur J Med Chem 238: (2022)
Nankai University
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Eur J Med Chem 238: (2022)
Stanford University
Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686.
Eur J Med Chem 238: (2022)
Southern Medical University
Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin receptor.
Bioorg Med Chem 66: (2022)
Rti International
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
J Med Chem 65: 7415-7437 (2022)
Nanjing University of Chinese Medicine
Discovery and Characterization of the First Nonpeptide Antagonists for the Relaxin-3/RXFP3 System.
J Med Chem 65: 7959-7974 (2022)
Research Triangle Institute
Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease.
Eur J Med Chem 238: (2022)
Chonnam National University
Ispinesib as an Effective Warhead for the Design of Autophagosome-Tethering Chimeras: Discovery of Potent Degraders of Nicotinamide Phosphoribosyltransferase (NAMPT).
J Med Chem 65: 7619-7628 (2022)
Second Military Medical University
Novel Quinoline Compounds as EZH2 Inhibitors for Treating Cancer.
ACS Med Chem Lett 13: 755-756 (2022)
Smith, Gambrell & Russell
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
ACS Med Chem Lett 13: 812-818 (2022)
Biocon Bristol Myers Squibb Research Center (Bbrc)
Indazole and Benzoisoxazole Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.
ACS Med Chem Lett 13: 763-764 (2022)
Smith, Gambrell & Russell
New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein-Protein Interaction.
ACS Med Chem Lett 13: 865-870 (2022)
H. Lee Moffitt Cancer Center and Research Institute
5-Oxopyrrolidine-3-carboxamides as Na
ACS Med Chem Lett 13: 761-762 (2022)
Smith, Gambrell & Russell
Novel Cyclic Cyanoenone Derivatives as KEAP1Modulators for Treating Neurodegenerative Diseases.
ACS Med Chem Lett 13: 777-778 (2022)
Smith, Gambrell & Russell
KRAS Inhibitors and Target Engagement Technology: From Undruggable to Druggable Targets in Cancer Therapeutics.
ACS Med Chem Lett 13: 752-754 (2022)
Usona Institute
2-Aminoquinazolines as LRRK2 Inhibitors for Treating Parkinson's Disease.
ACS Med Chem Lett 13: 775-776 (2022)
Smith, Gambrell & Russell
Novel CFTR Modulators for Treating Cystic Fibrosis.
ACS Med Chem Lett 13: 757-758 (2022)
Smith, Gambrell & Russell
Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles.
ACS Med Chem Lett 13: 848-854 (2022)
Riken Center For Sustainable Resource Science
3-Pyrrolidine-indole Derivatives as 5-HT2-Selective Receptor Modulators for the Potential Treatment of Mental Disorders.
ACS Med Chem Lett 13: 749-751 (2022)
Usona Institute
Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.
ACS Med Chem Lett 13: 841-847 (2022)
University of Nebraska Medical Center
Small-Molecule Inhibitor of the Oncogenic KRAS
ACS Med Chem Lett 13: 767-769 (2022)
Usona Institute
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
ACS Med Chem Lett 13: 779-785 (2022)
University of Copenhagen
Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies.
ACS Med Chem Lett 13: 819-826 (2022)
Yale University
Hybrids of polyphenolic acids and xanthone, the potential preventive and therapeutic effects on PD: Design, synthesis, in vitro anti-aggregation of α-synuclein, and disaggregation against the existed α-synuclein oligomer and fibril.
Bioorg Med Chem 66: (2022)
Zhengzhou University
Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-
J Med Chem 65: 7833-7842 (2022)
Jinan University
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABA
J Med Chem 65: 7876-7895 (2022)
Gedeon Richter
Biophysical Survey of Small-Molecule β-Catenin Inhibitors: A Cautionary Tale.
J Med Chem 65: 7246-7261 (2022)
University of Southampton
Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
Bioorg Med Chem Lett 70: (2022)
Ocean University of China
Design, synthesis and biological evaluation of chromone derivatives as novel protein kinase CK2 inhibitors.
Bioorg Med Chem Lett 69: (2022)
China Pharmaceutical University
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities.
Eur J Med Chem 238: (2022)
Sun Yat-Sen University
Highly Selective SERCA2a Activators: Preclinical Development of a Congeneric Group of First-in-Class Drug Leads against Heart Failure.
J Med Chem 65: 7324-7333 (2022)
University of Milano-Bicocca
Benzodiazepine Derivatives as Potent Vasopressin V
J Med Chem 65: 9295-9311 (2022)
Xuzhou Medical University
Discovery of Pentacyclic Triterpenoid PROTACs as a Class of Effective Hemagglutinin Protein Degraders.
J Med Chem 65: 7154-7169 (2022)
Peking University
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
Eur J Med Chem 238: (2022)
Shenyang Pharmaceutical University
Inhibition of cytochrome P450 monooxygenase-catalyzed oxylipin formation by flavonoids: Evaluation of structure-activity relationship towards CYP4F2-selective inhibitors.
Eur J Med Chem 238: (2022)
University of Wuppertal
2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands.
Bioorg Med Chem 66: (2022)
Uppsala University
Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
Bioorg Med Chem 66: (2022)
Tokyo Medical and Dental University
Design, synthesis and biological evaluation of novel indole derivatives as gut-selective NaPi2b inhibitors.
Bioorg Med Chem 66: (2022)
Taisho Pharmaceutical
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.
Bioorg Med Chem 66: (2022)
Shenyang Pharmaceutical University
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
ACS Med Chem Lett 13: 855-864 (2022)
University of Perugia
New pyrazole-tetrazole hybrid compounds as potent α-amylase and non-enzymatic glycation inhibitors.
Bioorg Med Chem Lett 69: (2022)
Mohamed 1St University
Targeting EZH2 for cancer therapy: From current progress to novel strategies.
Eur J Med Chem 238: (2022)
West China Hospital
Discovery of novel benzimidazole derivatives as potent p300 bromodomain inhibitors with anti-proliferative activity in multiple cancer cells.
Bioorg Med Chem 66: (2022)
Fudan University
Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
Eur J Med Chem 238: (2022)
Adam Mickiewicz University
Design, synthesis, and biological evaluation of trizole-based heteroaromatic derivatives as Bcr-Abl kinase inhibitors.
Eur J Med Chem 238: (2022)
Xi'An Jiaotong University
Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity.
Eur J Med Chem 238: (2022)
University of Sharjah
Identification, optimization, and biological evaluation of 3-O-β-chacotriosyl ursolic acid derivatives as novel SARS-CoV-2 entry inhibitors by targeting the prefusion state of spike protein.
Eur J Med Chem 238: (2022)
South China Agricultural University
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
Eur J Med Chem 238: (2022)
Hangzhou Medical College
Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors.
Eur J Med Chem 238: (2022)
Kafrelsheikh University
Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
Eur J Med Chem 238: (2022)
University of Siena
Angiotensin II AT2 receptor ligands with phenylthiazole scaffolds.
Bioorg Med Chem 65: (2022)
Uppsala University
Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein-Protein Interaction Inhibitors with an Alternative Binding Mode.
J Med Chem 65: 7380-7398 (2022)
University College London
Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine.
J Med Chem 65: 7682-7696 (2022)
University of Oxford
Tuaimenal A, a Meroterpene from the Irish Deep-Sea Soft Coral
J Nat Prod 85: 1315-1323 (2022)
University of South Florida
Preventing Influenza A Virus Infection by Mixed Inhibition of Neuraminidase and Hemagglutinin by Divalent Inhibitors.
J Med Chem 65: 7312-7323 (2022)
Utrecht University
Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma.
J Med Chem 65: 7278-7295 (2022)
Peking University
Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.
J Med Chem 65: 7170-7192 (2022)
Chiesi Farmaceutici
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
Eur J Med Chem 238: (2022)
China Pharmaceutical University
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
Bioorg Med Chem Lett 69: (2022)
Incyte Research Institute
Design, synthesis, and evaluation of new vanin-1 inhibitors based on RR6.
Bioorg Med Chem 65: (2022)
Osaka Medical and Pharmaceutical University
Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease
J Med Chem 65: 7334-7362 (2022)
Anhui Medical University
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
J Med Chem 65: 7212-7230 (2022)
University College London
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
J Med Chem 65: 7016-7043 (2022)
Affiliated Hospital of Guangdong Medical University
Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
Eur J Med Chem 238: (2022)
Institute For Medical Research and Occupational Health
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.
Eur J Med Chem 237: (2022)
Sapienza University of Rome
Design, synthesis and antitumor evaluation of novel 1H-indole-2-carboxylic acid derivatives targeting 14-3-3η protein.
Eur J Med Chem 238: (2022)
Tsinghua University
Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives.
J Med Chem 65: 7118-7140 (2022)
University of Pisa
Discovery and Structural Basis of the Selectivity of Potent Cyclic Peptide Inhibitors of MAGE-A4.
J Med Chem 65: 7231-7245 (2022)
University of North Carolina
Identification of novel indole derivatives as highly potent AMPK activators with anti-diabetic profiles.
Bioorg Med Chem Lett 68: (2022)
Shionogi
Optimization of 4-arylthiophene-3-carboxylic acid derivatives as inhibitors of ANO1: Lead optimization studies toward their analgesic efficacy for inflammatory pain.
Eur J Med Chem 237: (2022)
Peking University
Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP.
Eur J Med Chem 237: (2022)
Baylor College of Medicine
Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
Bioorg Med Chem 65: (2022)
Christian-Albrechts-University of Kiel
Electrostatic Complementarity in Structure-Based Drug Design.
J Med Chem 65: 7476-7488 (2022)
Astex Pharmaceuticals
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
J Med Chem 65: 7193-7211 (2022)
Guangzhou Institutes of Biomedicine and Health
Discovery of novel benzothiophene derivatives as potent and narrow spectrum inhibitors of DYRK1A and DYRK1B.
Bioorg Med Chem Lett 68: (2022)
Ach£
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Eur J Med Chem 237: (2022)
Nanjing University
Differential Modulation of Nuclear Receptor LRH-1 through Targeting Buried and Surface Regions of the Binding Pocket.
J Med Chem 65: 6888-6902 (2022)
Emory University School of Medicine
Design and synthesis of endocannabinoid enzyme inhibitors for ocular indications.
Bioorg Med Chem Lett 68: (2022)
Liberty University
Design, synthesis and conformation-activity relationship analysis of LNA/BNA-type 5'-O-aminoribosyluridine as MraY inhibitors.
Bioorg Med Chem 65: (2022)
Hokkaido University
New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production.
Eur J Med Chem 237: (2022)
Universidad De Granada
Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for mono-ADP-ribosyltransferases PARP10 and PARP15.
Eur J Med Chem 237: (2022)
University of Perugia
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
J Med Chem 65: 6573-6592 (2022)
Sun Yat-Sen University Cancer Center
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
J Med Chem 65: 6903-6925 (2022)
University of Cape Town
Discovery of Natural Ursane-type SENP1 Inhibitors and the Platinum Resistance Reversal Activity Against Human Ovarian Cancer Cells: A Structure-Activity Relationship Study.
J Nat Prod 85: 1248-1255 (2022)
Peking Union Medical College & Chinese Academy of Medical Sciences
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
J Med Chem 65: 8345-8379 (2022)
Novartis Institutes For Biomedical Research
Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain.
J Med Chem 65: 6656-6676 (2022)
University of Copenhagen
Recent advances in natural anti-obesity compounds and derivatives based on in vivo evidence: A mini-review.
Eur J Med Chem 237: (2022)
National Cheng Kung University
New Aβ(1-42) ligands from anti-amyloid antibodies: Design, synthesis, and structural interaction.
Eur J Med Chem 237: (2022)
University of Salerno
Discovery of indirubin-3'-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia.
Eur J Med Chem 237: (2022)
Gwangju Institute of Science and Technology
Lead optimization of pyrido[2,3-d][1]benzazepin-6-one derivatives leading to the discovery of a potent, selective, and orally available human parathyroid hormone receptor 1 (hPTHR1) antagonist (DS69910557).
Bioorg Med Chem 64: (2022)
Daiichi Sankyo
Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase.
Eur J Med Chem 237: (2022)
Central China Normal University
Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study.
Eur J Med Chem 237: (2022)
Shenyang Pharmaceutical University
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.
J Med Chem 65: 6390-6418 (2022)
The People'S Hospital of Xinjiang Uyghur Autonomous Region
In silico, synthesis and anticancer evaluation of benzamide tryptamine derivatives as novel eEF2K inhibitors.
Bioorg Med Chem Lett 67: (2022)
Ningbo University
Discovery of novel non-steroidal selective glucocorticoid receptor modulators by structure- and IGN-based virtual screening, structural optimization, and biological evaluation.
Eur J Med Chem 237: (2022)
Zhejiang University
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
Eur J Med Chem 237: (2022)
Federal University of Parana
A kind of HIV-1 protease inhibitors containing phenols with antiviral activity against DRV-resistant variants.
Bioorg Med Chem 64: (2022)
Chinese Academy of Medical Science and Peking Union Medical College
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.
J Med Chem 65: 11574-11606 (2022)
Institut De G£N£Tique Et De Biologie Mol£Culaire Et Cellulaire
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
J Med Chem 65: 6775-6802 (2022)
Schr£Dinger
Explorations of novel pyridine-pyrimidine hybrid phosphonate derivatives as aurora kinase inhibitors.
Bioorg Med Chem Lett 67: (2022)
Durgamata Institute of Pharmacy
Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis.
J Med Chem 65: 6710-6728 (2022)
East China Normal University
Occurrence, synthesis and biological activity of 2-(2-phenyethyl)chromones.
Eur J Med Chem 237: (2022)
Guizhou Medical University
Discovery of 3, 6-disubstituted isobenzofuran-1(3H)-ones as novel inhibitors of monoamine oxidases.
Bioorg Med Chem Lett 67: (2022)
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS
J Med Chem 65: 6940-6952 (2022)
Astrazeneca
Identification of Antithrombotic Natural Products Targeting the Major Substrate Binding Pocket of Protein Disulfide Isomerase.
J Nat Prod 85: 1332-1339 (2022)
Fuzhou University
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
Eur J Med Chem 237: (2022)
Collaborative Innovation Center of Functionalized Probes For Chemical Imaging In University of Shandong
Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
Eur J Med Chem 237: (2022)
Westf£Lische Wilhelms-Universit£T M£Nster
Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy.
Eur J Med Chem 237: (2022)
Zhuhai Campus of Zunyi Medical University
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
J Med Chem 65: 6513-6540 (2022)
Newcastle University Centre For Cancer
Development of Novel IP6K Inhibitors for the Treatment of Obesity and Obesity-Induced Metabolic Dysfunctions.
J Med Chem 65: 6869-6887 (2022)
University of North Carolina At Chapel Hill
Piezo-Type Mechanosensitive Ion Channel Component 1 (Piezo1): A Promising Therapeutic Target and Its Modulators.
J Med Chem 65: 6441-6453 (2022)
Shanghai Jiao Tong University
Dentithecamides A-H, Diacylated Zoanthoxanthin Derivatives with PAX3-FOXO1 Inhibitory Activity from the Hydroid
J Nat Prod 85: 1419-1427 (2022)
Yangzhou University
Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or naphthalene-N,N'-diacetic acids with varying C2-substituents as inhibitors of Keap1-Nrf2 protein-protein interaction.
Eur J Med Chem 237: (2022)
The State University of New Jersey
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
Eur J Med Chem 237: (2022)
Zhejiang University
Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
Eur J Med Chem 237: (2022)
University of Bari Aldo Moro
Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
Eur J Med Chem 236: (2022)
Universitat De Barcelona
Boron-Containing heterocycles as promising pharmacological agents.
Bioorg Med Chem 63: (2022)
Long Island University
Synthesis and evaluation of novel HER-2 inhibitors to exert anti-breast cancer ability through epithelial-mesenchymal transition (EMT) pathway.
Eur J Med Chem 237: (2022)
China Medical University
Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy.
J Med Chem 65: 6593-6611 (2022)
Southern Medical University
Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold.
ACS Med Chem Lett 13: 586-592 (2022)
China Pharmaceutical University
Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability.
ACS Med Chem Lett 13: 707-713 (2022)
The University of Kansas
Selective Macrocyclic Inhibitors of DYRK1A/B.
ACS Med Chem Lett 13: 577-585 (2022)
Dana-Farber Cancer Institute
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
ACS Med Chem Lett 13: 665-673 (2022)
Biogen
Factor XI Activation Inhibitors for Treating Thrombosis, Embolisms, Hypercoagulability, and Fibrotic Changes.
ACS Med Chem Lett 13: 530-531 (2022)
Smith, Gambrell & Russell
Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor.
ACS Med Chem Lett 13: 701-706 (2022)
Shanghai Hengrui Pharmaceutical
Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor.
ACS Med Chem Lett 13: 599-607 (2022)
Shenyang Pharmaceutical University
Discovery of Highly Potent Serotonin 5-HT
ACS Med Chem Lett 13: 648-657 (2022)
Northwestern University
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
ACS Med Chem Lett 13: 681-686 (2022)
Astrazeneca
Discovery and Evaluation of Novel Angular Fused Pyridoquinazolinonecarboxamides as RNA Polymerase I Inhibitors.
ACS Med Chem Lett 13: 608-614 (2022)
Johns Hopkins University
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy.
ACS Med Chem Lett 13: 528-529 (2022)
Smith, Gambrell & Russell
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.
ACS Med Chem Lett 13: 593-598 (2022)
Soochow University
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
ACS Med Chem Lett 13: 734-741 (2022)
Merck
Identification of Slow-Binding Inhibitors of the BoNT/A Protease.
ACS Med Chem Lett 13: 742-747 (2022)
The Scripps Research Institute
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an
ACS Med Chem Lett 13: 658-664 (2022)
Novartis Institutes For Biomedical Research
Discovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors.
ACS Med Chem Lett 13: 714-719 (2022)
Rigel Pharmaceuticals
Novel RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases.
ACS Med Chem Lett 13: 524-525 (2022)
Smith, Gambrell & Russell
Selective A
ACS Med Chem Lett 13: 623-631 (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.
ACS Med Chem Lett 13: 537-539 (2022)
Usona Institute
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
Eur J Med Chem 236: (2022)
Universit£
New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold.
Eur J Med Chem 237: (2022)
University of Turin
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.
Eur J Med Chem 237: (2022)
Nankai University
Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer.
Bioorg Med Chem Lett 67: (2022)
Sichuan University
The evaluation of N-propargylamine-2-aminotetralin as an inhibitor of monoamine oxidase.
Bioorg Med Chem Lett 67: (2022)
North-West University
Discovery of a Novel Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) and Cyclin-Dependent Kinase 4 (CDK4) Dual Inhibitor for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 65: 6729-6747 (2022)
China Pharmaceutical University
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
J Med Chem 65: 6840-6858 (2022)
Jinan University
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.
J Med Chem 65: 6803-6825 (2022)
West China Hospital of Sichuan University
Discovery of First-in-Class TAK1-MKK3 Protein-Protein Interaction (PPI) Inhibitor
J Med Chem 65: 6690-6709 (2022)
Fudan University
Structure-Based Design of a Novel Class of Autotaxin Inhibitors Based on Endogenous Allosteric Modulators.
J Med Chem 65: 6338-6351 (2022)
University of Strathclyde
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Bioorg Med Chem 63: (2022)
Astrazeneca
The Ascension of Targeted Covalent Inhibitors.
J Med Chem 65: 5886-5901 (2022)
University of Massachusetts Medical School
Potent Inhibition of SARS-CoV-2 nsp14 
J Med Chem 65: 6231-6249 (2022)
University of Montpellier
Novel Sphingosine Kinase 1 Inhibitor Suppresses Growth of Solid Tumor and Inhibits the Lung Metastasis of Triple-Negative Breast Cancer.
J Med Chem 65: 7697-7716 (2022)
China Pharmaceutical University
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na
Bioorg Med Chem 63: (2022)
Abbvie
Overview of SIRT5 as a potential therapeutic target: Structure, function and inhibitors.
Eur J Med Chem 236: (2022)
China Pharmaceutical University
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
Eur J Med Chem 236: (2022)
Shenyang Pharmaceutical University
The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery.
Eur J Med Chem 237: (2022)
University of Helsinki
Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes.
Eur J Med Chem 237: (2022)
Shanghaitech University
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).
Bioorg Med Chem Lett 66: (2022)
Wuxi Apptec
Stapled peptides as scaffolds for developing radiotracers for intracellular targets: Preliminary evaluation of a radioiodinated MDM2-binding stapled peptide in the SJSA-1 osteosarcoma model.
Bioorg Med Chem Lett 66: (2022)
Duke University Medical Center
Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization.
J Med Chem 65: 6287-6312 (2022)
Frederick National Laboratory For Cancer Research
Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance.
J Med Chem 65: 6017-6038 (2022)
Korea University
Recent advancements in chromone as a privileged scaffold towards the development of small molecules for neurodegenerative therapeutics.
RSC Med Chem 13: 258-279 (2022)
Jamia Millia Islamia
Recent advances in the discovery of protein tyrosine phosphatase SHP2 inhibitors.
RSC Med Chem 13: 246-257 (2022)
Soochow University
Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression.
Eur J Med Chem 236: (2022)
East China University of Science and Technology
Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer.
Eur J Med Chem 236: (2022)
West China Hospital of Sichuan University
Modular synthesis of 2,4-diaminoanilines as CNS drug-like non-covalent inhibitors of asparagine endopeptidase.
Bioorg Med Chem 63: (2022)
University of Florence
Pyrazolones as inhibitors of immune checkpoint blocking the PD-1/PD-L1 interaction.
Eur J Med Chem 236: (2022)
Univ. Lille
Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Eur J Med Chem 236: (2022)
Anhui Medical University
Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles.
Eur J Med Chem 236: (2022)
China Pharmaceutical University
Discovery of 4-((E)-3,5-dimethoxy-2-((E)-2-nitrovinyl)styryl)aniline derivatives as potent and orally active NLRP3 inflammasome inhibitors for colitis.
Eur J Med Chem 236: (2022)
School of Pharmacy Anhui Medical University
Identification of Aloe-derived natural products as prospective lead scaffolds for SARS-CoV-2 main protease (M
Bioorg Med Chem Lett 66: (2022)
University of Colorado
Novel Selective Galectin-3 Antagonists Are Cytotoxic to Acute Lymphoblastic Leukemia.
J Med Chem 65: 5975-5989 (2022)
Griffith University
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
J Med Chem 65: 6325-6337 (2022)
Jinan University
Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
Eur J Med Chem 236: (2022)
Guangdong University of Technology
Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.
Bioorg Med Chem Lett 66: (2022)
Wuxi Apptec
Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells.
J Med Chem 65: 6207-6230 (2022)
Shanghai Institute of Materia Medica
Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor.
J Med Chem 65: 6070-6087 (2022)
Universitat Ramon Llull
Targeting the Aryl Hydrocarbon Receptor with Microbial Metabolite Mimics Alleviates Experimental Colitis in Mice.
J Med Chem 65: 6859-6868 (2022)
Palack£
Topoisomerase I inhibitors: Challenges, progress and the road ahead.
Eur J Med Chem 236: (2022)
Csir-Indian Institute of Chemical Biology
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor.
Bioorg Med Chem Lett 66: (2022)
Cadila Healthcare
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Bioorg Med Chem Lett 66: (2022)
Daiichi Sankyo
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR
Bioorg Med Chem Lett 72: (2022)
Shanghai Institute of Materia Medica
Demonstration of a Common DPhe
J Med Chem 65: 5990-6000 (2022)
University of Michigan
Synthesis and Pharmacological Evaluation of New
J Med Chem 65: 6250-6260 (2022)
Hospital Universitario Santa Cristina
Advancements in the development of multi-target directed ligands for the treatment of Alzheimer's disease.
Bioorg Med Chem 61: (2022)
Central University of Punjab
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.
Eur J Med Chem 236: (2022)
Ningxia Medical University
Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment.
Bioorg Med Chem Lett 66: (2022)
Southern Medical University
Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Eur J Med Chem 236: (2022)
Jagiellonian University Medical College
Synthesis of heterocyclic ring-fused analogs of HMG499 as novel degraders of HMG-CoA reductase that lower cholesterol.
Eur J Med Chem 236: (2022)
East China Normal University
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
Eur J Med Chem 235: (2022)
University of Texas At Austin
Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.
Eur J Med Chem 236: (2022)
University of Chinese Academy of Sciences
Polyphenolic compounds: Synthesis, assessment of antimicrobial effect and enzymes inhibition against important medicinal enzymes with computational details.
Bioorg Med Chem Lett 65: (2022)
Bartin University
Development of inhibitors targeting glycogen synthase kinase-3β for human diseases: Strategies to improve selectivity.
Eur J Med Chem 236: (2022)
West China Hospital
Dual-acting antitumor agents targeting the A
Eur J Med Chem 236: (2022)
Shanghaitech University
Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury.
Eur J Med Chem 236: (2022)
Sun Yat-Sen University
Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy.
Eur J Med Chem 236: (2022)
School of Pharmaceutical Sciences
Development of novel dipeptide nitriles as inhibitors of rhodesain of Trypanosoma brucei rhodesiense.
Eur J Med Chem 236: (2022)
University of Messina
Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Eur J Med Chem 236: (2022)
Yancheng Teachers University
Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors.
Eur J Med Chem 236: (2022)
Guangzhou Medical University
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Bioorg Med Chem Lett 68: (2022)
Dana-Farber Cancer Institute
Proteostasis Regulators in Cystic Fibrosis: Current Development and Future Perspectives.
J Med Chem 65: 5212-5243 (2022)
University of Bologna
4,5-Dihydroxypyrimidine Methyl Carboxylates, Carboxylic Acids, and Carboxamides as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease.
J Med Chem 65: 5830-5849 (2022)
University of Minnesota
New N-aryl-N'-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT
Eur J Med Chem 235: (2022)
Cracow University of Technology
Recent results from non-basic glycosidase inhibitors: How structural diversity can inform general strategies for improving inhibition potency.
Eur J Med Chem 235: (2022)
University of Newcastle
6-Aryl-quinazolines as novel GABA
Bioorg Med Chem Lett 67: (2022)
Chemical Works of Gedeon Richter
Recent advances in the development of active hybrid molecules in the treatment of cardiovascular diseases.
Bioorg Med Chem 62: (2022)
Western University of Health Sciences
Discovery of small-molecule inhibitors of RUVBL1/2 ATPase.
Bioorg Med Chem 62: (2022)
California Institute of Technology
Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors.
Bioorg Med Chem Lett 67: (2022)
Jiangnan University
Design, Synthesis, and Proof-of-Concept of Triple-Site Inhibitors against Aminoacyl-tRNA Synthetases.
J Med Chem 65: 5800-5820 (2022)
Sun Yat-Sen University
Long Residence Time at the Vasopressin V
J Med Chem 65: 7717-7728 (2022)
Xuzhou Medical University
Discovery of a Highly Selective β
J Med Chem 65: 5514-5527 (2022)
Shenyang Pharmaceutical University
Synthesis and biological evaluation of glucagon-like peptide-1 analogs with the C-terminal helix 3 of albumin-binding domain 3.
Bioorg Med Chem 62: (2022)
China State Institute of Pharmaceutical Industry
Discovery and biological evaluation of tanshinone derivatives as potent dual inhibitors of indoleamine 2, 3-dioxygenase 1 and tryptophan 2, 3-dioxygenase.
Eur J Med Chem 235: (2022)
Kunming Institute of Botany
Discovery of Thieno[2,3-
J Med Chem 65: 5724-5750 (2022)
Shanghai Institute of Materia Medica
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.
J Med Chem 65: 6499-6512 (2022)
Shionogi
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
J Med Chem 65: 5317-5333 (2022)
Novartis Institutes For Biomedical Research
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
J Med Chem 65: 5575-5592 (2022)
TBA
Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for "Diabesity".
J Med Chem 65: 5449-5461 (2022)
Hospital Regional Universitario
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
J Med Chem 65: 5660-5674 (2022)
Cnrs
Design, synthesis and biological evaluation of novel pyridine derivatives as gut-selective NaPi2b inhibitors.
Bioorg Med Chem Lett 65: (2022)
Taisho Pharmaceutical
Pyrrolidinyl benzofurans and benzodioxanes: Selective α4β2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.
Bioorg Med Chem Lett 65: (2022)
Universit£
A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.
Nature (2022)
University of British Columbia
An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials.
Eur J Med Chem 235: (2022)
Jouf University
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles.
Eur J Med Chem 235: (2022)
Adam Mickiewicz University
Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease.
Eur J Med Chem 235: (2022)
China Pharmaceutical University
Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations.
Eur J Med Chem 235: (2022)
University of Palermo
Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity.
Eur J Med Chem 235: (2022)
Fudan University
HR1405-01, a Safe intravenous NSAID with superior anti-inflammatory and analgesic activities in preclinical trials.
Eur J Med Chem 235: (2022)
China Pharmaceutical University
Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.
Bioorg Med Chem 61: (2022)
Friedrich-Alexander Universit£T Erlangen-N£Rnberg
Thiosemicarbazone derivatives: Evaluation as cruzipain inhibitors and molecular modeling study of complexes with cruzain.
Bioorg Med Chem 61: (2022)
Universidad De Buenos Aires
Structure-Based Discovery and Optimization of Furo[3,2-
J Med Chem 65: 5760-5799 (2022)
Chinese Academy of Sciences
A Series of Substituted Bis-Aminotriazines Are Activators of the Natriuretic Peptide Receptor C.
J Med Chem 65: 5495-5513 (2022)
University College London
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
J Med Chem 65: 5675-5689 (2022)
Merck
A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
Eur J Med Chem 235: (2022)
Universit£?Degli Studi Di Bari "Aldo Moro
Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity.
Eur J Med Chem 235: (2022)
Eberhard Karls Universit£T
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
J Med Chem 65: 5184-5211 (2022)
Sichuan University
Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.
J Med Chem 65: 5334-5354 (2022)
Shanghai Pharmaceuticals Holding
Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.
Bioorg Med Chem Lett 64: (2022)
Southern Research
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
J Med Chem 65: 5407-5432 (2022)
Korea Research Institute of Chemical Technology
Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine.
Eur J Med Chem 235: (2022)
Ku Leuven
Principles of Kinase Allosteric Inhibition and Pocket Validation.
J Med Chem 65: 5288-5299 (2022)
Relay Therapeutics
Covalent sortase A inhibitor ML346 prevents
RSC Med Chem 13: 138-149 (2022)
Shanghai Institute of Materia Medica
Design, synthesis, and biological evaluation of C
RSC Med Chem 13: 175-182 (2022)
Allegheny General Hospital
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
RSC Med Chem 13: 202-207 (2022)
Washington University
Structure-activity relationships of valine,
RSC Med Chem 13: 156-174 (2022)
The University of Sydney
Inhibition of N-type calcium ion channels by tricyclic antidepressants - experimental and theoretical justification for their use for neuropathic pain.
RSC Med Chem 13: 183-195 (2022)
The University of Queensland
Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective.
Eur J Med Chem 235: (2022)
Shenyang Pharmaceutical University
A novel photocaged B-Raf
Bioorg Med Chem Lett 64: (2022)
Shanghai Institute of Organic Chemistry
Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.
J Med Chem 65: 5244-5273 (2022)
University of South Australia
Design, synthesis, and biological evaluation of novel 2'-methyl-2'-fluoro-6-methyl-7-alkynyl-7-deazapurine nucleoside analogs as anti-Zika virus agents.
Eur J Med Chem 234: (2022)
Guangzhou Institutes of Biomedicine and Health
Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
Eur J Med Chem 234: (2022)
Martin-Luther University of Halle-Wittenberg
Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
Eur J Med Chem 234: (2022)
Isf College of Pharmacy
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.
Bioorg Med Chem Lett 64: (2022)
Chinese Academy of Sciences
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases.
Eur J Med Chem 234: (2022)
National Institute of Pharmaceutical Education and Research (NIPER)
Recent applications of vinyl sulfone motif in drug design and discovery.
Eur J Med Chem 234: (2022)
Mazandaran University of Medical Sciences
Design and development of photoswitchable DFG-Out RET kinase inhibitors.
Eur J Med Chem 234: (2022)
University of Gothenburg
Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors.
Eur J Med Chem 234: (2022)
China Pharmaceutical University
Synthesis and Profiling of Highly Selective Inhibitors of Methyltransferase DOT1L Based on Carbocyclic C-Nucleosides.
J Med Chem 65: 5701-5723 (2022)
Masaryk University
Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).
J Med Chem 65: 5300-5316 (2022)
Principia Biopharma, A Sanofi
Malaria Box-Inspired Discovery of
ACS Med Chem Lett 13: 365-370 (2022)
Virginia Tech
Structure-Activity Relationship of Anti-
ACS Med Chem Lett 13: 417-427 (2022)
Martin-Luther-Universit£T Halle-Wittenberg
Development of Myostatin Inhibitory d-Peptides to Enhance the Potency, Increasing Skeletal Muscle Mass in Mice.
ACS Med Chem Lett 13: 492-498 (2022)
Tokyo University of Pharmacy and Life Sciences
Novel Tricyclic Heteroaryl Compounds as IRAK4 Inhibitors for Treating Cancer, Autoimmune and Inflammatory Diseases.
ACS Med Chem Lett 13: 336-337 (2022)
Smith, Gambrell & Russell
Discovery of SHR5133, a Highly Potent and Novel HBV Capsid Assembly Modulator.
ACS Med Chem Lett 13: 507-512 (2022)
Shanghai Hengrui Pharmaceutical
Identification of the Highly Active, Species Cross-Reactive Complex I Inhibitor BAY-179.
ACS Med Chem Lett 13: 348-357 (2022)
Bayer
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
ACS Med Chem Lett 13: 475-482 (2022)
St. Jude Children'S Research Hospital
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors.
ACS Med Chem Lett 13: 377-387 (2022)
Tri-Institutional Therapeutics Discovery Institute
Dual Reversible Coumarin Inhibitors Mutually Bound to Monoamine Oxidase B and Acetylcholinesterase Crystal Structures.
ACS Med Chem Lett 13: 499-506 (2022)
Swedish Defence Research Agency
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series.
Eur J Med Chem 234: (2022)
University of Ljubljana
Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis.
J Med Chem 65: 5539-5564 (2022)
Shenyang Pharmaceutical University
Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
Bioorg Med Chem 60: (2022)
Indian Institute of Technology (Banaras Hindu University)
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
ACS Med Chem Lett 13: 457-462 (2022)
Takeda Pharmaceutical
Discovery of Pyridone-Substituted Triazolopyrimidine Dual A
ACS Med Chem Lett 13: 436-442 (2022)
Fudan University
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.
J Med Chem 65: 4600-4615 (2022)
Agios Pharmaceuticals
Aspulvins A-H, Aspulvinone Analogues with SARS-CoV-2 M
J Nat Prod 85: 878-887 (2022)
Yunnan University
Structure-activity relationship studies of functionalized aromatic peptidomimetics as neurolysin activators.
Bioorg Med Chem Lett 64: (2022)
University of Nebraska Medical Center
Design, synthesis, and biological evaluation of polyphenol derivatives as DYRK1A inhibitors. The discovery of a potentially promising treatment for Multiple Sclerosis.
Bioorg Med Chem Lett 64: (2022)
Avanti Biosciences
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase.
Eur J Med Chem 234: (2022)
University of Gothenburg
SAR of Novel 3-Arylisoquinolinones:
J Med Chem 65: 4783-4797 (2022)
University of Manchester
Virtual screening and crystallographic studies reveal an unexpected γ-lactone derivative active against MptpB as a potential antitubercular agent.
Eur J Med Chem 234: (2022)
University of Milan
Identification of N, C-capped di- and tripeptides as selective immunoproteasome inhibitors.
Eur J Med Chem 234: (2022)
Chinese Academy of Medical Sciences and Peking Union Medical College
Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification.
Eur J Med Chem 234: (2022)
University of Palermo
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
J Med Chem 65: 4972-4990 (2022)
Amgen Research
Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis.
Eur J Med Chem 234: (2022)
China Pharmaceutical University
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.
Eur J Med Chem 234: (2022)
Peking Union Medical College and Chinese Academy of Medical Sciences
Chemical synthesis and pharmacological properties of heparin pentasaccharide analogues.
Eur J Med Chem 234: (2022)
Chinese Academy of Sciences
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
Eur J Med Chem 234: (2022)
Yantai University
Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C.
Eur J Med Chem 233: (2022)
Chinese Academy of Medical Sciences and Peking Union Medical College
Natural products and synthetic analogues against HIV: A perspective to develop new potential anti-HIV drugs.
Eur J Med Chem 233: (2022)
University of Belgrade
Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
Eur J Med Chem 233: (2022)
"G. D'Annunzio" University of Chieti-Pescara
Discovery of Thieno[2,3-d]pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening.
Eur J Med Chem 233: (2022)
Southern Medical University
Rational design, synthesis, antiproliferative activity against MCF-7, MDA-MB-231 cells, estrogen receptors binding affinity, and computational study of indenopyrimidine-2,5-dione analogs for the treatment of breast cancer.
Bioorg Med Chem Lett 64: (2022)
Comsats University Islamabad
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.
Bioorg Med Chem Lett 63: (2022)
Eternity Bioscience
Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva.
Bioorg Med Chem Lett 64: (2022)
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of 7H-pyrrolo [2,3-d] pyrimidine derivatives as potential p21-activated kinase 4 (PAK4) inhibitors.
Bioorg Med Chem 60: (2022)
China Pharmaceutical University
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
Bioorg Med Chem Lett 64: (2022)
Shenyang Pharmaceutical University
Optimization of a Pyrimidinone Series for Selective Inhibition of Ca
J Med Chem 65: 4667-4686 (2022)
Purdue University
Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease.
J Med Chem 65: 4909-4925 (2022)
University of Barcelona (Ub)
Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
J Med Chem 65: 5113-5133 (2022)
Jinan University
Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.
Eur J Med Chem 233: (2022)
Henan University
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
J Med Chem 65: 4534-4564 (2022)
Bristol-Myers Squibb
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.
Eur J Med Chem 233: (2022)
Wenzhou Medical University
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Ureidopropanamides as Formyl Peptide Receptor 2 (FPR2) Agonists to Target the Resolution of Inflammation in Central Nervous System Disorders.
J Med Chem 65: 5004-5028 (2022)
Universit£
Design, Synthesis, and Biological Evaluation of NAP Isosteres: A Switch from Peripheral to Central Nervous System Acting Mu-Opioid Receptor Antagonists.
J Med Chem 65: 5095-5112 (2022)
Virginia Commonwealth University
Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.
J Med Chem 65: 4991-5003 (2022)
Virginia Commonwealth University
Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
Bioorg Med Chem 60: (2022)
Sichuan University
Design, synthesis and glycosidase inhibition of C-4 branched LAB and DAB derivatives.
Eur J Med Chem 233: (2022)
Chinese Academy of Sciences
Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
Eur J Med Chem 233: (2022)
Shenyang Pharmaceutical University
A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning.
J Med Chem 65: 4649-4666 (2022)
Institut De Recherche Biom£Dicale Des Arm£Es
Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome.
J Med Chem 65: 5029-5043 (2022)
China Pharmaceutical University
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
Eur J Med Chem 233: (2022)
Jagiellonian University Medical College
Recent development of BTK-based dual inhibitors in the treatment of cancers.
Eur J Med Chem 233: (2022)
Nantong University
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
Eur J Med Chem 233: (2022)
China Pharmaceutical University
Small-molecule inhibitors targeting small ubiquitin-like modifier pathway for the treatment of cancers and other diseases.
Eur J Med Chem 233: (2022)
China Pharmaceutical University
Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
Eur J Med Chem 233: (2022)
China Pharmaceutical University
Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors.
Bioorg Med Chem Lett 63: (2022)
Sichuan University
Antibacterial activity evaluation of vinyl sulfones against global predominant methicillin-resistant Staphylococcus aureus USA300.
Bioorg Med Chem Lett 63: (2022)
Mahidol University
Jatrophane Diterpenoids with Kv1.3 Ion Channel Inhibitory Effects from
J Nat Prod 85: 815-827 (2022)
Huazhong University of Science and Technology
Resveratrol-Based MTDLs to Stimulate Defensive and Regenerative Pathways and Block Early Events in Neurodegenerative Cascades.
J Med Chem 65: 4727-4751 (2022)
Instituto De Qu£Mica M£Dica
Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer.
J Med Chem 65: 4878-4892 (2022)
Gifu Pharmaceutical University
Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation.
J Med Chem 65: 4403-4423 (2022)
Stanford University
Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma.
J Med Chem 65: 5374-5391 (2022)
Wenzhou Medical University
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.
J Med Chem 65: 6001-6016 (2022)
Pharmaron Beijing
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
J Med Chem 65: 4818-4831 (2022)
Second Military Medical University
Development of Sulfamoylated 4-(1-Phenyl-1
J Med Chem 65: 5044-5056 (2022)
Gdask University of Technology
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
J Med Chem 65: 6356-6389 (2022)
Hefei University of Technology
Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs.
J Med Chem 65: 4949-4971 (2022)
Viiv Healthcare
Discovery of Potential Neuroprotective Agents against Paclitaxel-Induced Peripheral Neuropathy.
J Med Chem 65: 4767-4782 (2022)
National Cheng Kung University
Discovery of novel ataxia telangiectasia mutated (ATM) kinase modulators: Computational simulation, biological evaluation and cancer combinational chemotherapy study.
Eur J Med Chem 233: (2022)
Peking University
Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents.
Eur J Med Chem 233: (2022)
Jiangsu Normal University
Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.
Bioorg Med Chem Lett 65: (2022)
Redx Anti-Infectives
Discovery of 4-phenylindolines containing a (5-cyanopyridin-3-yl)methoxy moiety as potent inhibitors of the PD-1/PD-L1 interaction.
Bioorg Med Chem Lett 63: (2022)
Shenyang Pharmaceutical University
Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation.
Bioorg Med Chem Lett 63: (2022)
Jiangnan University
Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.
J Med Chem 65: 3923-3942 (2022)
Shanghai Institute of Materia Medica
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
J Med Chem 65: 3798-3813 (2022)
Novartis Institutes For Biomedical Research
Discovery of novel 2,8-diazaspiro[4.5]decan-1-one derivatives as potent RIPK1 kinase inhibitors.
Bioorg Med Chem 59: (2022)
China Pharmaceutical University
Discovery of dual-target ligands binding to beta2-adrenoceptor and cysteinyl-leukotriene receptor for the potential treatment of asthma from natural products derived DNA-encoded library.
Eur J Med Chem 233: (2022)
Northwest University
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
RSC Med Chem 13: 79-89 (2022)
The Hong Kong Polytechnic University
Insights into the modular design of kinase inhibitors and application to Abl and Axl.
RSC Med Chem 13: 64-71 (2022)
University of Michigan
An overview of the development of EED inhibitors to disable the PRC2 function.
RSC Med Chem 13: 39-53 (2022)
University of Jinany
Targeting the S2 Subsite Enables the Structure-Based Discovery of Novel Highly Selective Factor XIa Inhibitors.
J Med Chem 65: 4318-4334 (2022)
Hefei University of Technology
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme.
Eur J Med Chem 232: (2022)
Universidade De Santiago De Compostela
Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity.
Bioorg Med Chem 59: (2022)
Astellas Pharma
A score years' update in the synthesis and biological evaluation of medicinally important 2-pyridones.
Eur J Med Chem 232: (2022)
Chaudhary Charan Singh Haryana Agricultural University
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.
Eur J Med Chem 233: (2022)
Zhejiang University
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
Bioorg Med Chem Lett 62: (2022)
University of Wisconsin-Milwaukee
Discovery and optimization of betulinic acid derivatives as novel potent CD73 inhibitors.
Bioorg Med Chem 59: (2022)
The Second Military Medical University
Discovery of Anticancer Agents of Diverse Natural Origin.
J Nat Prod 85: 702-719 (2022)
University of Illinois At Chicago
Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8
J Med Chem 65: 4367-4386 (2022)
Fudan University
Expansion of the 4-(Diethylamino)benzaldehyde Scaffold to Explore the Impact on Aldehyde Dehydrogenase Activity and Antiproliferative Activity in Prostate Cancer.
J Med Chem 65: 3833-3848 (2022)
University of Bradford
Medicines for millions of patients.
RSC Med Chem 13: 7-12 (2022)
Astex Pharmaceuticals
Recent insight into the biological activities and SAR of quinolone derivatives as multifunctional scaffold.
Bioorg Med Chem 59: (2022)
Maharishi Markandeshwar (Deemed To Be University)
Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.
J Med Chem 65: 3758-3775 (2022)
National Clinical Research Center For Geriatrics
Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
J Med Chem 65: 4335-4349 (2022)
Shanghai Institute of Materia Medica
Telocinobufagin Has Antitumor Effects in Non-Small-Cell Lung Cancer by Inhibiting STAT3 Signaling.
J Nat Prod 85: 765-775 (2022)
Wenzhou Medical University
Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
J Med Chem 65: 4350-4366 (2022)
Aurigene Discovery Technologies
Probing Fluorinated Motifs onto Dual AChE-MAO B Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Early-ADME Studies.
J Med Chem 65: 3962-3977 (2022)
University of Bari "Aldo Moro
Structure-Based Design of a Chemical Probe Set for the 5-HT
J Med Chem 65: 4201-4217 (2022)
University of California
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.
J Med Chem 65: 3991-4006 (2022)
Shanghai Institute of Materia Medica
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.
J Med Chem 65: 3849-3865 (2022)
Zhejiang University
Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain.
J Med Chem 65: 4182-4200 (2022)
Moffitt Cancer Center
Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease.
Bioorg Med Chem 58: (2022)
Universidad De Navarra
Design and synthesis of novel spirocyclic carboxylic acids as potent and orally bioavailable DGAT1 inhibitors and their biological evaluation.
Bioorg Med Chem Lett 62: (2022)
Dr.Vishwanath Karad Mit World Peace University
Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore.
J Med Chem 65: 4270-4290 (2022)
Takeda Pharmaceutical
-Aryl Mercaptopropionamides as Broad-Spectrum Inhibitors of Metallo-β-Lactamases.
J Med Chem 65: 3913-3922 (2022)
Helmholtz Institute For Pharmaceutical Research Saarland
Discovery and Structural Optimization of Toddacoumalone Derivatives as Novel PDE4 Inhibitors for the Topical Treatment of Psoriasis.
J Med Chem 65: 4238-4254 (2022)
National-Local Joint Engineering Laboratory of Druggability and New Drugs Evaluation
Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation.
J Med Chem 65: 3879-3893 (2022)
China Pharmaceutical University
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
J Med Chem 65: 4007-4017 (2022)
Universit£
The Design and Optimization of Monomeric Multitarget Peptides for the Treatment of Multifactorial Diseases.
J Med Chem 65: 3685-3705 (2022)
China Pharmaceutical University
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against
J Med Chem 65: 4255-4269 (2022)
University of California San Diego
Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.
Eur J Med Chem 232: (2022)
Sichuan University
Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis.
Eur J Med Chem 232: (2022)
Sichuan University
Discovery of novel 3-butyl-6-benzyloxyphthalide Mannich base derivatives as multifunctional agents against Alzheimer's disease.
Bioorg Med Chem 58: (2022)
Sichuan University
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
Eur J Med Chem 232: (2022)
Shenyang Pharmaceutical University
Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach.
Eur J Med Chem 232: (2022)
Tanta University
Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir.
Bioorg Med Chem Lett 62: (2022)
Australian National University
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1
J Med Chem 65: 4291-4317 (2022)
Bristol Myers Squibb
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
J Med Chem 65: 4058-4084 (2022)
Emory University
Hydrophobic Tagging-Induced Degradation of PDEδ in Colon Cancer Cells.
ACS Med Chem Lett 13: 298-303 (2022)
Second Military Medical University
Proteome-wide Identification of Off-Targets of a Potent EGFR
ACS Med Chem Lett 13: 292-297 (2022)
University of Macau
Exploring Non-orthosteric Interactions with a Series of Potent and Selective A
ACS Med Chem Lett 13: 243-249 (2022)
Universidade De Santiago De Compostela
Increased Molecular Flexibility Widens the Gap between
ACS Med Chem Lett 13: 211-217 (2022)
Okayama University Graduate School of Medicine
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR
ACS Med Chem Lett 13: 196-202 (2022)
Jinan University
Novel Aminocyclobutanes as Monoacylglycerol Lipase Modulators.
ACS Med Chem Lett 13: 162-163 (2022)
Smith, Gambrell & Russell
Novel Difluorocyclohexyl Derivatives as IL-17 Modulators for Treating Inflammatory and Autoimmune Diseases.
ACS Med Chem Lett 13: 160-161 (2022)
Smith, Gambrell & Russell
Biaryl Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).
ACS Med Chem Lett 13: 158-159 (2022)
Smith, Gambrell & Russell
Novel Isoindolone Compounds as HPK1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 13: 156-157 (2022)
Smith, Gambrell & Russell
Factor XI Activation Inhibitors for Treating Thrombosis, Embolisms, Hypercoagulability, and Fibrotic Changes.
ACS Med Chem Lett 13: 154-155 (2022)
Smith, Gambrell & Russell
Small molecules targeting γ-secretase and their potential biological applications.
Eur J Med Chem 232: (2022)
Shenyang Pharmaceutical University
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
J Med Chem 65: 3786-3797 (2022)
TBA
Drug Repurposing of Quisinostat to Discover Novel
J Med Chem 65: 4156-4181 (2022)
East China University of Science and Technology
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
J Med Chem 65: 3729-3757 (2022)
Shandong University
Stereo-Defined Acyclic Nucleoside Phosphonates are Selective and Potent Inhibitors of Parasite 6-Oxopurine Phosphoribosyltransferases.
J Med Chem 65: 4030-4057 (2022)
The Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
J Med Chem 65: 4121-4155 (2022)
Bristol Myers Squibb
Human Neuraminidases: Structures and Stereoselective Inhibitors.
J Med Chem 65: 3002-3025 (2022)
Universit£
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
J Med Chem 65: 3173-3192 (2022)
Eberhard Karls University T£Bingen
Drugging the Next Undruggable KRAS Allele-Gly12Asp.
J Med Chem 65: 3119-3122 (2022)
University of California San Francisco
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.
J Med Chem 65: 3134-3150 (2022)
Mcgill University
Discovery of Novel 3-Piperidinyl Pyridine Derivatives as Highly Potent and Selective Cholesterol 24-Hydroxylase (CH24H) Inhibitors.
J Med Chem 65: 3343-3358 (2022)
Takeda Pharmaceutical
Activable Targeted Protein Degradation Platform Based on Light-triggered Singlet Oxygen.
J Med Chem 65: 3632-3643 (2022)
Wuhan University of Science and Technology
Structure-activity relationships of N-terminal variants of peptidomimetic tissue transglutaminase inhibitors.
Eur J Med Chem 232: (2022)
University of Ottawa
Phe19 modification of HDM2-p53 PPI inhibitors to alleviate CYP3A4 metabolism/mechanism-based inhibition liability.
Bioorg Med Chem Lett 61: (2022)
Merck
Strategies Targeting Protein Tyrosine Phosphatase SHP2 for Cancer Therapy.
J Med Chem 65: 3066-3079 (2022)
Zhengzhou University
Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor.
J Med Chem 65: 3098-3118 (2022)
University of Camerino
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
J Med Chem 65: 3667-3683 (2022)
Shandong University
Interaction of A
Eur J Med Chem 231: (2022)
National Cancer Institute (Ba, Mm, Sl, Sva)
Novel potent benzimidazole-based microsomal prostaglandin E
Eur J Med Chem 231: (2022)
Gazi University
Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists.
Bioorg Med Chem Lett 61: (2022)
University of Nebraska Medical Center
A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion.
Bioorg Med Chem Lett 61: (2022)
University of Miami
Recent advances of human dihydroorotate dehydrogenase inhibitors for cancer therapy: Current development and future perspectives.
Eur J Med Chem 232: (2022)
West China Hospital
Discovery of indol-6-yl-pyrrolo[2,3-c]pyridin-7-one derivatives as bromodomain-containing protein 4 (BRD4) inhibitors for the treatment of kidney fibrosis.
Eur J Med Chem 231: (2022)
West China Hospital of Sichuan University
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
J Med Chem 65: 3080-3097 (2022)
University of Naples "Federico Ii
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
J Med Chem 65: 3359-3370 (2022)
University of Cambridge
Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library.
J Med Chem 65: 3597-3605 (2022)
Sun Yat-Sen University Cancer Center
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
Eur J Med Chem 232: (2022)
Shaoxing University
Discovery of pyrroledione analogs as potent transient receptor potential canonical channel 5 inhibitors.
Bioorg Med Chem Lett 61: (2022)
China Pharmaceutical University
Discovery and Optimization of Highly Selective Inhibitors of CDK5.
J Med Chem 65: 3575-3596 (2022)
Goldfinc Bio
Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.
J Med Chem 65: 3229-3248 (2022)
Zhejiang University
Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
Eur J Med Chem 231: (2022)
Mazandaran University of Medical Sciences
Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
Bioorg Med Chem 57: (2022)
Georgia Institute of Technology
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
J Med Chem 65: 3306-3331 (2022)
Astrazeneca
Development of a Novel, Small-Molecule Brain-Penetrant Histone Deacetylase Inhibitor That Enhances Spatial Memory Formation in Mice.
J Med Chem 65: 3388-3403 (2022)
University of Wisconsin-Milwaukee
NAE modulators: A potential therapy for gastric carcinoma.
Eur J Med Chem 231: (2022)
Southwest Jiaotong University
Building on endogenous lipid mediators to design synthetic receptor ligands.
Eur J Med Chem 231: (2022)
The University of Tokyo
Design and synthesis of pyrido[2,3-d]pyrimidine derivatives for a novel PAC1 receptor antagonist.
Eur J Med Chem 231: (2022)
University of Toyama
A fragment integrational approach to GPCR inhibition: Identification of a high affinity small molecule CXCR4 antagonist.
Eur J Med Chem 231: (2022)
Tsinghua University
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 61: (2022)
Shaoxing University
Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors.
Bioorg Med Chem Lett 60: (2022)
Palack£
Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.
Eur J Med Chem 231: (2022)
Comsats University Islamabad
Identification of triazolopyridine derivatives as a new class of AhR agonists and evaluation of anti-psoriasis effect in a mouse model.
Eur J Med Chem 231: (2022)
Sichuan University
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease.
Bioorg Med Chem 57: (2022)
Irbm
Recent applications of seven-membered rings in drug design.
Bioorg Med Chem 57: (2022)
Evotec (U.K.)
Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators.
Bioorg Med Chem Lett 61: (2022)
Cerevance
Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability.
Bioorg Med Chem 57: (2022)
Fudan University
Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies.
J Med Chem 65: 3644-3666 (2022)
Icahn School of Medicine At Mount Sinai
Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors.
J Med Chem 65: 3249-3265 (2022)
Jinan University
Discovery of HDAC6-Selective Inhibitor NN-390 with
J Med Chem 65: 3193-3217 (2022)
University of Toronto Mississauga
In silico screening-based discovery of novel covalent inhibitors of the SARS-CoV-2 3CL protease.
Eur J Med Chem 231: (2022)
Shanghai Institute of Materia Medica
Phage display-based discovery of cyclic peptides against the broad spectrum bacterial anti-virulence target CsrA.
Eur J Med Chem 231: (2022)
Institute For Pharmaceutical Research Saarland (Hips)
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics.
J Med Chem 65: 3420-3433 (2022)
University of South Carolina
Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition.
J Med Chem 65: 3371-3387 (2022)
University of Cape Town
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
J Med Chem 65: 3434-3459 (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Identification of a Novel 2,8-Diazaspiro[4.5]decan-1-one Derivative as a Potent and Selective Dual TYK2/JAK1 Inhibitor for the Treatment of Inflammatory Bowel Disease.
J Med Chem 65: 3151-3172 (2022)
Sichuan University and Collaborative Innovation Center of Biotherapy
Discovery of Dimeric Arylsulfonamides as Potent ADAM8 Inhibitors.
ACS Med Chem Lett 12: 1787-1793 (2021)
University of Pisa
Probing Embryonic Development Enables the Discovery of Unique Small-Molecule Bone Morphogenetic Protein Potentiators.
J Med Chem 65: 3978-3990 (2022)
Technical University Dortmund
Discovery of Non-Nucleotide Small-Molecule STING Agonists
J Med Chem 65: 3518-3538 (2022)
Bristol Myers Squibb Research and Development
Importance of Binding Site Hydration and Flexibility Revealed When Optimizing a Macrocyclic Inhibitor of the Keap1-Nrf2 Protein-Protein Interaction.
J Med Chem 65: 3473-3517 (2022)
Uppsala University
Development of dihydropyrrolopyridinone-based PKN2/PRK2 chemical tools to enable drug discovery.
Bioorg Med Chem Lett 60: (2022)
University of Sussex
Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from
J Nat Prod 85: 453-457 (2022)
South-Central University For Nationalities
Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents.
Eur J Med Chem 231: (2022)
Mansoura University
Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
Eur J Med Chem 231: (2022)
Hangzhou Normal University
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
Eur J Med Chem 231: (2022)
Peking Union Medical College and Chinese Academy of Medical Sciences
Neuropeptide B/W receptor 1 peptidomimetic agonists: Structure-activity relationships and plasma stability.
Eur J Med Chem 231: (2022)
Rti International
Discovery of Pteridine-7(8
J Med Chem 65: 2694-2709 (2022)
East China University of Science and Technology
Unique Oxidative Metabolism of Bufalin Generates Two Reactive Metabolites That Strongly Inactivate Human Cytochrome P450 3A.
J Med Chem 65: 4018-4029 (2022)
Shanghai University of Traditional Chinese Medicine
Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs.
Eur J Med Chem 231: (2022)
Sanquan College of Xinxiang Medical University
Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond.
Eur J Med Chem 231: (2022)
China Pharmaceutical University
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.
Eur J Med Chem 230: (2022)
China Pharmaceutical University
Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
Bioorg Med Chem Lett 60: (2022)
West China School of Pharmacy Sichuan University
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
J Med Chem 65: 1961-1978 (2022)
University of Toronto
Synthesis and Characterization of 5-(2-Fluoro-4-[
J Med Chem 65: 2593-2609 (2022)
Harvard Medical School
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1).
J Med Chem 65: 2174-2190 (2022)
Chinese Academy of Sciences
Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for Neuroimaging.
J Med Chem 65: 2191-2207 (2022)
Eth Zurich
Multivalent peptide dendrimers inhibit the fusion of viral-cellular membranes and the cellular NF-κB signaling pathway.
Eur J Med Chem 230: (2022)
The Third Affiliated Hospital of Guangzhou Medical University
Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB
J Med Chem 65: 2374-2387 (2022)
National Institute On Alcohol Abuse and Alcoholism
Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
J Med Chem 65: 4218-4237 (2022)
Shandong University
Target-Based Virtual Screening and LC/MS-Guided Isolation Procedure for Identifying Phloroglucinol-Terpenoid Inhibitors of SARS-CoV-2.
J Nat Prod 85: 327-336 (2022)
Kunming Institute of Botany
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.
J Med Chem 65: 2313-2328 (2022)
Chinese Academy of Sciences
Illuminating a Dark Kinase: Structure-Guided Design, Synthesis, and Evaluation of a Potent Nek1 Inhibitor and Its Effects on the Embryonic Zebrafish Pronephros.
J Med Chem 65: 1265-1282 (2022)
Technische Universit£T Darmstadt
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
J Med Chem 65: 1536-1551 (2022)
University of Arkansas For Medical Sciences
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6
J Med Chem 65: 2035-2058 (2022)
Sichuan University
Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.
J Med Chem 65: 2409-2433 (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Tigliane Diterpenoids with Larvicidal, Antifungal, and α-Glucosidase Inhibitory Activities from
J Nat Prod 85: 405-414 (2022)
Yunnan University of Chinese Medicine
Discovery of 4-(phenoxymethyl)-1H-1,2,3-triazole derivatives as novel xanthine oxidase inhibitors.
Bioorg Med Chem Lett 60: (2022)
China Medical University
Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
J Med Chem 65: 2471-2496 (2022)
Mcgill University
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
J Med Chem 65: 3539-3562 (2022)
Korea Institute of Science & Technology (Kist)
-Substituted 5-(1
J Med Chem 65: 1979-1995 (2022)
Mirea Russian Technological University
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived
J Nat Prod 85: 337-344 (2022)
The University of Queensland
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
J Med Chem 65: 2122-2138 (2022)
Fudan University
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A
J Med Chem 65: 2091-2106 (2022)
Universidade De Santiago De Compostela
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore.
J Med Chem 65: 2610-2622 (2022)
The University of Queensland
Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides.
Bioorg Med Chem Lett 59: (2022)
Bolu Abant ?Zzet Baysal University
Design, synthesis and biological evaluation of novel 1H-pyrazole-4-carbonyl-4,5,6,7-tetrahydrobenzo [b]thiophene derivatives as gut-selective NaPi2b inhibitors.
Bioorg Med Chem Lett 59: (2022)
Taisho Pharmaceutical
Synthesis of tropane-based σ
Eur J Med Chem 230: (2022)
Westf£Lische Wilhelms-Universit£T M£Nster
Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
Eur J Med Chem 230: (2022)
Anhui Medical University
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Bioorg Med Chem Lett 59: (2022)
Genentech
A kinase inhibitor which specifically targets the ABL myristate pocket (STAMP), but unlike asciminib crosses the blood-brain barrier.
Bioorg Med Chem Lett 59: (2022)
Novartis Institutes For Biomedical Research
Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 60: (2022)
Nanyang Normal University
Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors.
Bioorg Med Chem 56: (2022)
Tokyo Medical and Dental University
Discovery and mechanistic study of thiazole-4-acylsulfonamide derivatives as potent and orally active ChemR23 inhibitors with a long-acting effect in cynomolgus monkeys.
Bioorg Med Chem 56: (2022)
Kyowa Kirin
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).
Eur J Med Chem 230: (2022)
China Pharmaceutical University
Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors.
Eur J Med Chem 230: (2022)
Zhengzhou University
Niemann-Pick C1-Like 1 inhibitors for reducing cholesterol absorption.
Eur J Med Chem 230: (2022)
The Affiliated Hospital of Qingdao University
Identification of novel xanthine oxidase inhibitors via virtual screening with enhanced characterization of molybdopterin binding groups.
Eur J Med Chem 230: (2022)
Chinese Academy of Medical Sciences and Peking Union Medical College
Roles and drug development of METTL3 (methyltransferase-like 3) in anti-tumor therapy.
Eur J Med Chem 230: (2022)
Yunnan University
Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.
Eur J Med Chem 230: (2022)
Chinese Academy of Sciences
Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
Bioorg Med Chem Lett 59: (2022)
Shionogi
Cell-based screening of extracts of natural sources to search for inhibitors of the ubiquitin-proteasome system and identification of proteasome inhibitors from the fungus Remotididymella sp.
Bioorg Med Chem Lett 59: (2022)
Kumamoto University
BOPPY-based novel fluorescent dopamine D
Bioorg Med Chem Lett 59: (2022)
Heinrich Heine University D£Sseldorf
Diaryl triazenes inhibit cytochrome P450 1A1 and 1B1 more strongly than aryl morpholino triazenes.
Bioorg Med Chem Lett 59: (2022)
Whittier College
Development of Novel Dihydrofuro[3,4-
J Med Chem 65: 2458-2470 (2022)
Shandong University
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis.
J Med Chem 65: 2571-2592 (2022)
China Pharmaceutical University
Discovery and Optimization of 7-Alkylidenyltetrahydroindazole-Based Acylsulfonamide EP3 Antagonists.
ACS Med Chem Lett 13: 111-117 (2022)
Janssen Research & Development
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
ACS Med Chem Lett 13: 84-91 (2022)
Genentech
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
ACS Med Chem Lett 13: 76-83 (2022)
Janssen Research & Development
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators.
ACS Med Chem Lett 13: 55-62 (2022)
Pfizer
Novel Macrocyclic Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors.
ACS Med Chem Lett 13: 27-28 (2022)
Smith, Gambrell & Russell
Novel Macrocyclic LRRK2 Inhibitors for Treating Parkinson's Disease.
ACS Med Chem Lett 13: 25-26 (2022)
Smith, Gambrell & Russell
Therapeutic Potential of Monoacylglycerol Lipase (MGL) Inhibitors as Treatment for Pain, Depression, Cancers, and Eye Conditions.
ACS Med Chem Lett 13: 22-24 (2022)
Therachem Research Medilab
The Inhibitors of Protein Tyrosine Phosphatase Nonreceptor Type 2 (PTPN2) as Potential Enhancers of Cancer Immunotherapy and Type 1 (PTPN1) as Treatment of Metabolic Diseases.
ACS Med Chem Lett 13: 19-21 (2022)
Therachem Research Medilab
Cyclic ADP Ribose Hydrolase (CD38) Inhibitors.
ACS Med Chem Lett 13: 13-14 (2022)
Temple University
A Series of Pyrazole Analogs Binding to KRASG12C as Potential Cancer Treatment.
ACS Med Chem Lett 13: 11-12 (2022)
Arrival Discovery
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
Bioorg Med Chem 56: (2022)
Guangdong Pharmaceutical University
Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity.
Bioorg Med Chem 56: (2022)
Takeda Pharmaceutical
Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists.
Eur J Med Chem 230: (2022)
National and Kapodistrian University of Athens
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.
Eur J Med Chem 230: (2022)
Hubei Polytechnic University
Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs.
Bioorg Med Chem Lett 59: (2022)
University of Minnesota
Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring.
Bioorg Med Chem Lett 60: (2022)
University of Tsukuba
Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Bioorg Med Chem Lett 59: (2022)
Daiichi Sankyo
Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors.
Bioorg Med Chem Lett 61: (2022)
China Pharmaceutical University
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.
ACS Med Chem Lett 13: 92-98 (2022)
Sunovion Pharmaceuticals
In Vitro and In Vivo Inhibition of the
J Med Chem 65: 1996-2022 (2022)
University of North Carolina At Chapel Hill
Discovery of Novel Histone Deacetylase 6 (HDAC6) Inhibitors with Enhanced Antitumor Immunity of Anti-PD-L1 Immunotherapy in Melanoma.
J Med Chem 65: 2434-2457 (2022)
Southern Medical University
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
Bioorg Med Chem 56: (2022)
Nanchang University
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
Bioorg Med Chem Lett 60: (2022)
Biogen
Essential structure of orexin 1 receptor antagonist YNT-707: Conversion of the 16-cyclopropylmethyl group to the 16-sulfonamide group in d-nor-nalfurafine derivatives.
Bioorg Med Chem Lett 59: (2022)
University of Tsukuba
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of
J Med Chem 65: 1749-1766 (2022)
Mirati Therapeutics
Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry.
ACS Med Chem Lett 12: 228-235 (2021)
William S. Middleton Veterans Hospital
Discovery of Gut-Restricted Small-Molecule Inhibitors of Intestinal Sodium-Dependent Phosphate Transport Protein 2b (NaPi2b) for the Treatment of Hyperphosphatemia.
J Med Chem 65: 1946-1960 (2022)
Kyowa Kirin
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.
Bioorg Med Chem 56: (2022)
Ain Shams University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Bioorg Med Chem 56: (2022)
Indian Institute of Technology (B.H.U.)
Synthesis of 8-aminomorphans with high KOR affinity.
Eur J Med Chem 230: (2022)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
Eur J Med Chem 230: (2022)
Peking Union Medical College & Chinese Academy of Medical Sciences
Design and synthesis of Osthole-based compounds as potential Nrf2 agonists.
Bioorg Med Chem Lett 61: (2022)
East China University of Science and Technology
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
J Med Chem 65: 1915-1932 (2022)
Korea University
Functionalized resorcinarenes effectively disrupt the aggregation of αA66-80 crystallin peptide related to cataracts.
RSC Med Chem 12: 2022-2030 (2021)
Oakland University
Synthesis of low-molecular weight fucoidan derivatives and their binding abilities to SARS-CoV-2 spike proteins.
RSC Med Chem 12: 2016-2021 (2021)
Keio University
An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases.
RSC Med Chem 12: 2001-2015 (2021)
Universidade Federal Do Rio Grande Do Sul Av. Bento
Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.
Eur J Med Chem 230: (2022)
Guizhou Medical University
Medicinal chemistry of the myeloid C-type lectin receptors Mincle, Langerin, and DC-SIGN.
RSC Med Chem 12: 1985-2000 (2021)
Heinrich-Heine-University of D�Sseldorf
Design, synthesis and biological evaluation of simplified analogues of MraY inhibitory natural product with rigid scaffold.
Bioorg Med Chem 55: (2022)
Tokyo University of Agriculture and Technology
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Eur J Med Chem 230: (2022)
Universit£
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.
J Med Chem 65: 1662-1684 (2022)
Csir-Indian Institute of Chemical Biology
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.
Eur J Med Chem 230: (2022)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of P2-modified proline analogues targeting the HtrA serine protease in Chlamydia.
Eur J Med Chem 230: (2022)
University of Otago
Design and synthesis of novel orexin 2 receptor agonists based on naphthalene skeleton.
Bioorg Med Chem Lett 59: (2022)
University of Tsukuba
Novel benzothiazole-based dual VEGFR-2/EGFR inhibitors targeting breast and liver cancers: Synthesis, cytotoxic activity, QSAR and molecular docking studies.
Bioorg Med Chem Lett 58: (2022)
National Research Centre
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
Bioorg Med Chem Lett 59: (2022)
University of Tsukuba
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
J Med Chem 65: 2342-2360 (2022)
University of Minnesota
-Methylpropargylamine-Conjugated Hydroxamic Acids as Dual Inhibitors of Monoamine Oxidase A and Histone Deacetylase for Glioma Treatment.
J Med Chem 65: 2208-2224 (2022)
University of Southern California
Curated by BindingDB
Curated by ChEMBL