137 articles for B Li
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Article Title
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Discovery of new Syk inhibitors through structure-based virtual screening.
Second Military Medical University
Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
Key Laboratory of The Ministry of Education For Medicinal Resources and Natural Pharmaceutical Chemistry
Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Merck Research Laboratories
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Abbvie
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.
Chinese Academy of Sciences
Separation and peroxisome proliferator-activated receptor-¿ agonist activity evaluation of synthetic racemic bavachinin enantiomers.
Shanghai University of Traditional Chinese Medicine
Rapid development of two factor IXa inhibitors from hit to lead.
Merck Research Laboratories
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.
Alcon Laboratories
Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.
Activx Biosciences
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Pfizer
Identification of unique VLA-4 antagonists from a combinatorial library.
Merck Research Laboratories
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.
Merck Research Laboratories
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Abbott Laboratories
Coumarin-based inhibitors of Bacillus anthracis and Staphylococcus aureus replicative DNA helicase: chemical optimization, biological evaluation, and antibacterial activities.
Microbiotix
An efficient synthesis of 3-OBn-6ß,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.
University of New England
Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors.
Microbiotix
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Abbott Laboratories
Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections.
Pfizer
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.
Sichuan University
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Neurocrine Biosciences
Synthesis and inhibitory activity of oligosaccharide thiazolines as a class of mechanism-based inhibitors for endo-beta-N-acetylglucosaminidases.
University of Maryland
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
Georgetown University Medical Center
A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization
TBA
6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3ß: discovery of nitrile derivatives with picomolar potency.
Activx Biosciences
Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3ß.
Activx Biosciences
Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists.
Lundbeck Research Usa
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
Pfizer
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Chinese Academy of Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.
Neurocrine Biosciences
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Abbott Bioresearch Center
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
Ocean University of China
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.
Sun Yat-Sen University
Design, synthesis and biological evaluation of N-salicyloyl tryptamine derivatives as multifunctional neuroprotectants for the treatment of ischemic stroke.
University of South China
Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.
Chinese Academy of Sciences
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Sun Yat-Sen University
Design, synthesis and structure-activity relationship of 1,8-naphthalimide derivatives as highly potent hCYP1B1 inhibitors.
Nanjing University of Chinese Medicine
Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents.
Wenzhou Medical University
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Pharmaron UK Ltd.
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Lundbeck Research Usa
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Lundbeck Research Usa
Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.
Henan University of Chinese Medicine
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Shanghai Institute of Materia Medica
Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.
Sun Yat-Sen University
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
South China University
Tuning the Metabolic Stability of Visual Cycle Modulators through Modification of an RPE65 Recognition Motif.
University of California - Irvine
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.
Sun Yat-Sen University
Discovery of quinazoline HPK1 inhibitors with high cellular potency.
Emd Serono Research & Development Institute
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase.
Shanghai University of Traditional Chinese Medicine
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells.
Peking University
Discovery of thienopyridines as Src-family selective Lck inhibitors.
Abbott Bioresearch Center
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.
Tufts University School of Medicine
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Merck Research Laboratories
Discovery of pyrrolo[2,3-d]pyrimidine-based molecules as a Wee1 inhibitor template.
Capital Medical University
Discovery and development of selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors.
China Pharmaceutical University
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Abbott Bioresearch Center
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Activx Biosciences
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.
Chinese Academy of Sciences
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.
Abbott Bioresearch Center
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
University of North Carolina at Chapel Hill
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.
Fujian Medical University
Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
Sun Yat-Sen University
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity.
China Pharmaceutical University
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.
Chinese Academy of Sciences
Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y
China Pharmaceutical University
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
Nankai University
Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators.
Xiamen University
Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth invitro and invivo.
East China University of Science and Technology
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.
National Cancer Institute-Frederick
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.
National Institutes of Health
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Moffitt Cancer Center
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Merck Research Laboratories
Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma.
University of Paris
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.
Sichuan University
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.
Dana-Farber Cancer Institute
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Merck Research Laboratories
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors.
China Pharmaceutical University
Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents.
Bengbu Medical College
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.
Biogen
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.
High Magnetic Field Laboratory
Design and synthesis of novel conformationally restricted HIV protease inhibitors.
Vertex Pharmaceuticals
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
Vertex Pharmaceuticals
Design, synthesis and anti-inflammatory evaluation of 3-amide benzoic acid derivatives as novel P2Y
China Pharmaceutical University
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors.
Peking University
Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus.
Peking University
Discovery of candesartan cilexetic as a novel neddylation inhibitor for suppressing tumor growth.
Shanghai University of Traditional Chinese Medicine
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
Northwest University
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
Jinan University
Flavonoids from Matteuccia struthiopteris and Their Anti-influenza Virus (H1N1) Activity.
Shenyang Pharmaceutical University
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: design, synthesis and evaluation as antibacterial agent.
Jishou University
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.
Chinese Academy of Sciences
Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PA
South China Agricultural University
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Unc Eshelman School of Pharmacy
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa
Xenon Pharmaceuticals
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
East China University of Science and Technology
Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design.
Shenyang Pharmaceutical University
Novel 4-arylaminoquinazoline derivatives with (E)-propen-1-yl moiety as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
Shaanxi Normal University
Discovery of the selective and efficacious inhibitors of FLT3 mutations.
China Pharmaceutical University
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.
Lilly Research Laboratories
Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors.
Anhui Medical University
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
Shaanxi Normal University
Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
East China University of Science and Technology
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.
China Pharmaceutical University
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR andα-glucosidase.
Key Laboratory of The Ministry of Education For Medicinal Resources and Natural Pharmaceutical Chemistry
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
East China University of Science and Technology
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
East China University of Science and Technology
PYRIDO[4,3-b]INDOLE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Ventus Therapeutics U.S.
Fluorescent antagonists of the A3 adenosine receptor
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.
Gwangju Institute of Science and Technology
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors
Leo Pharma
Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
Merck Patent
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.
Merck Research Laboratories
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.
University of Zimbabwe