121 articles for C Yang
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Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.
Second Military Medical University
Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
China Pharmaceutical University
Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.
Second Military Medical University
Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.
The Scripps Research Institute
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.
Second Military Medical University
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
Ocean University of China
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Merck
Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors.
The Scripps Research Institute
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
TBA
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Chinese Academy of Sciences
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Tianjin University of Science and Technology
Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening.
East China University of Science and Technology
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
Nankai University
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.
Peking Union Medical College
Building predictive models for protein tyrosine phosphatase 1B inhibitors based on discriminating structural features by reassembling medicinal chemistry building blocks.
Leadscope
Finding discriminating structural features by reassembling common building blocks.
Leadscope
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
TBA
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines.
The State University of New Jersey
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Merck Research Laboratories
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
Chinese Academy of Sciences
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Neurocrine Biosciences
Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.
Neurocrine Biosciences
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.
Neurocrine Biosciences
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
Johnson & Johnson Pharmaceutical Research & Development
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Neurocrine Biosciences
Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia.
Fudan University
Discovery of a high potent PIM kinase inhibitor for acute myeloid leukemia based on N-pyridinyl amide scaffold by optimizing the fragments toward to Lys67 and Asp128/Glu171.
Fudan University
Discovery of new tetrahydroisoquinolines as potent and selective LSD1 inhibitors for the treatment of MLL-rearranged leukemia.
Zhejiang Ocean University
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Sun Yat-Sen University
Allosteric Activation of α7 Nicotinic Acetylcholine Receptors by Novel 2-Arylamino-thiazole-5-carboxylic Acid Amide Derivatives for the Improvement of Cognitive Deficits in Mice.
Qingdao University Medical College
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.
Zunyi Medical University
Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma.
Shanghai Institute of Materia Medica
Design, synthesis, and biological evaluation of 3-phenyl substituted pyridine derivatives as potential dual inhibitors of XOR and URAT1.
South China University of Technology
Novel berberine derivatives as p300 histone acetyltransferase inhibitors in combination treatment for breast cancer.
Sichuan University
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation.
Fudan University
Recent two-year advances in anti-dengue small-molecule inhibitors.
Macao University of Science and Technology
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.
Nankai University
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP.
Sun Yat-Sen University
Discovery, Synthesis, and Evaluation of Novel Dual Inhibitors of a Vascular Endothelial Growth Factor Receptor and Poly(ADP-Ribose) Polymerase for BRCA Wild-Type Breast Cancer Therapy.
Sichuan University
Identification and in silicon binding study of a novel NR2B selective NMDAR antagonist.
Shenyang Pharmaceutical University
Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ inhibitors for hematological cancer.
Fudan University
Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.
Chengdu Anticancer Bioscience
Simplified staurosporine analogs as potent JAK3 inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.
West China Hospital of Sichuan 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.
West China Hospital of Sichuan University
Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
The Affiliated Hospital of Southwest Medical University
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.
Chinese Academy of Sciences
Repurposing old drugs as novel inhibitors of human MIF from structural and functional analysis.
Wuhan University
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Wyeth Research
Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand.
Shanghai Institute of Traumatology and Orthopaedics
Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B.
J. Michael Bishop Institute of Cancer Research
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Chinese Academy of Sciences
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
Sichuan University
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Chinese Academy of Sciences
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity.
Soochow University
Peptidylarginine deiminases 4 as a promising target in drug discovery.
Zhejiang Ocean University
Identification of Novel Fused Heteroaromatics-Based MALT1 Inhibitors by High-Throughput Screening to Treat B Cell Lymphoma.
Chinese Academy of Sciences
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.
Fudan University
Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.
West China Hospital of Sichuan University
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.
Fudan University
Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of
Chinese Academy of Sciences
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
Nankai University
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
Nankai University
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Merck
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Merck Research Laboratories
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.
Huazhong University of Science & Technology
Discovery of Clinical Candidate (5-(3-(4-Chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an Orally Bioavailable Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.
China Pharmaceutical University
Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors.
Northwest A&F University
Development of Small-Molecules Targeting Receptor Activator of Nuclear Factor-κB Ligand (RANKL)-Receptor Activator of Nuclear Factor-κB (RANK) Protein-Protein Interaction by Structure-Based Virtual Screening and Hit Optimization.
Shanghai Jiaotong University School of Medicine
Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.
Tianjin University of Science and Technology
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
Chinese Academy of Sciences
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Fudan University
Discovery of 3,3'-Spiro[Azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection.
Wuxi Apptec (Shanghai) Co.
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Merck
TGF-B INHIBITOR COMPOUND AND USE THEREOF
Medinno Pharmaceutical Technology (Zhuhai) Co.
CARBOXYLIC ACID-CONTAINING COMPOUNDS AS MODULATORS OF BIS-PHOSPHOGLYCERATE MUTASE FOR THE TREATMENT OF SICKLE CELL DISEASE
Genzyme
Process for the synthesis of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one
Imara
3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
Board of Trustees of The Southern Illinois University
Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity
Kancera
2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides
Pfizer
Substituted piperidine compounds and their use as orexin receptor modulators
Janssen Pharmaceutica
Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
Janssen Pharmaceutica
Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Smithkline Beecham Pharmaceuticals
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Glaxosmithkline