127 articles for Y Luo
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Article Title
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Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
Pfizer
Identification of Potential Off-target Toxicity Liabilities of Catechol-O-methyltransferase Inhibitors by Differential Competition Capture Compound Mass Spectrometry.
Caprotec Bioanalytics
Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.
University of South Florida
An Orally Available BACE1 Inhibitor That Affords Robust CNS Aß Reduction without Cardiovascular Liabilities.
Amgen
New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase.
Institute of Pharmacology and Toxicology
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
Sun Yat-Sen University
Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design.
Shanghai Jiao Tong University
Discovery of 2-methylpyridine-based biaryl amides as¿-secretase modulators for the treatment of Alzheimer's disease.
Amgen
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
East China Normal University
Indazoles as potential c-Met inhibitors: design, synthesis and molecular docking studies.
Guangdong Pharmaceutical University
Synthesis, biological evaluation, and molecular docking studies of novel 1,3,4-oxadiazole derivatives possessing benzotriazole moiety as FAK inhibitors with anticancer activity.
Nanjing University
The discovery of colchicine-SAHA hybrids as a new class of antitumor agents.
East China Normal University
Synthesis, biological evaluation, 3D-QSAR studies of novel aryl-2H-pyrazole derivatives as telomerase inhibitors.
Nanjing University
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.
Amgen
2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.
Shanghai Jiao Tong University
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.
Abbott Laboratories
Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents.
Sichuan University
Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.
University of South Carolina
Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.
Nanjing University
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
Nanjing University
The development of N-a-(2-carboxyl)benzoyl-N(5)-(2-fluoro-1-iminoethyl)-l-ornithine amide (o-F-amidine) and N-a-(2-carboxyl)benzoyl-N(5)-(2-chloro-1-iminoethyl)-l-ornithine amide (o-Cl-amidine) as second generation protein arginine deiminase (PAD) inhibitors.
The Scripps Research Institute
Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.
Nanjing University
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Amgen
Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
East China Normal University
Discovery of vinylogous carbamates as a novel class ofß-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors.
Soochow University
Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors.
Nanjing University
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Abbott Laboratories
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Abbott Laboratories
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Abbott Laboratories
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Abbott Laboratories
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
Ocean University of China
Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity.
Sichuan University
Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo.
Sichuan University
Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus.
Sichuan University
Discovery of a Novel Series of Homo sapiens Caseinolytic Protease P Agonists for Colorectal Adenocarcinoma Treatment via ATF3-Dependent Integrated Stress Response.
Sichuan University
Facilitating the development of molecular glues: Opportunities from serendipity and rational design.
Sichuan University
Discovery of 5-(Piperidin-4-yl)-1,2,4-oxadiazole Derivatives as a New Class of Human Caseinolytic Protease P Agonists for the Treatment of Hepatocellular Carcinoma.
Sichuan University
Discovery and Optimization of Novel SaFabI Inhibitors as Specific Therapeutic Agents for MRSA Infection.
Sichuan University
Exploration of novel isoxazole-fused quinone derivatives as anti-colorectal cancer agents through inhibiting STAT3 and elevating ROS level.
Sichuan University
Strategies for the Discovery of Oxazolidinone Antibacterial Agents: Development and Future Perspectives.
Sichuan University
Structure-Activity Relationship of Novel Pyrimidine Derivatives with Potent Inhibitory Activities against
Sichuan University
Discovery of a dual-acting inhibitor of interleukin-1β and STATs for the treatment of inflammatory bowel disease.
Guangzhou Medical University
Discovery of potent human dihydroorotate dehydrogenase inhibitors based on a benzophenone scaffold.
Sichuan University
Therapeutic potential of targeting kynurenine pathway in neurodegenerative diseases.
Shaoxing University
Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases.
Graduate School of Chinese Academy of Sciences
Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
Sichuan University
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.
Sichuan University
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
Aventis Pharmaceuticals
Design, Synthesis, and Biological Evaluation of a Novel Series of Teriflunomide Derivatives as Potent Human Dihydroorotate Dehydrogenase Inhibitors for Malignancy Treatment.
Sichuan University
Structure-Guided Design of the First Noncovalent Small-Molecule Inhibitor of CRM1.
Sichuan University and Collaborative Innovation Centre of Biotherapy
Discovery of 3-aryl substituted benzoxaboroles as broad-spectrum inhibitors of serine- and metallo-β-lactamases.
Sichuan University
Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.
Southeast University
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.
Cullgen (Shanghai)
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
Glutamyl-gamma-boronate inhibitors of bacterial Glu-tRNA(Gln) amidotransferase.
Dupont Pharmaceuticals
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
Sun Yat-Sen University
Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers
Sichuan University
A novel series of napabucasin derivatives as orally active inhibitors of signal transducer and activator of transcription 3 (STAT3).
Sichuan University
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Shenyang Pharmaceutical University
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.
East China University of Science & Technology
Optimization of substituted cinnamic acyl sulfonamide derivatives as tubulin polymerization inhibitors with anticancer activity.
Second Military Medical University
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Sichuan University
Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Shenyang Pharmaceutical University
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Wuxi Apptec
Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold.
Sun Yat-Sen University
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
West China Hospital
FAK DEGRADERS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS
Berrybio (Shanghai)
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of heart failure and disorders related thereto
Arena Pharmaceuticals
1H-IMIDAZO [4,5-H] QUINAZOLINE COMPOUND AS NOVEL SELECTIVE FLT3 INHIBITORS
Shengke Pharmaceuticals (Jiangsu)
Dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof
Topadur Pharma
Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity
Kancera
3-oxa-8-azabicyclo[3.2.1]octane derivatives and their use in the treatment of cancer and hemoglobinopathies
Ctxt
Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones
Dart Neuroscience (Cayman)
3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof
Merck Sharp & Dohme
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.
Shandong University
Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.
Ataturk University
Affinity Selection-Mass Spectrometry Identifies a Novel Antibacterial RNA Polymerase Inhibitor.
Merck
SF2312 is a natural phosphonate inhibitor of enolase.
University of Texas M. D. Anderson Cancer Center
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.
Pfizer
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
National Institutes of Health
Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes.
University of Dundee
9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.
Hoechst-Roussel Pharmaceuticals
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
Merck Research Laboratories
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Merck Research Laboratories