123 articles for C Yang
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PMID
Cmpds
Data
Article Title
Organization
33
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
21
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
3
Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.
Second Military Medical University
16
Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.
The Scripps Research Institute
13
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.
Second Military Medical University
10
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
Ocean University of China
33
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
29
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Merck
8
Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors.
The Scripps Research Institute
38
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
TBA
29
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Chinese Academy of Sciences
22
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
25
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Tianjin University of Science and Technology
15
Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening.
East China University of Science and Technology
77
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
33
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
Nankai University
26
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.
Peking Union Medical College
59
Building predictive models for protein tyrosine phosphatase 1B inhibitors based on discriminating structural features by reassembling medicinal chemistry building blocks.
Leadscope
16
Finding discriminating structural features by reassembling common building blocks.
Leadscope
4
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
37
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
TBA
7
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines.
The State University of New Jersey
38
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
26
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Merck Research Laboratories
9
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
5
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Neurocrine Biosciences
25
Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.
Neurocrine Biosciences
27
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.
Neurocrine Biosciences
8
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
15
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
Johnson & Johnson Pharmaceutical Research & Development
24
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Neurocrine Biosciences
2
Identification of a RANKL/TNF-α Dual-Inhibitor as a Potential Disease-Modifying Agent for the Treatment of Knee Osteoarthritis.
ShanghaiTech University
41
Design, synthesis, and evaluation of chalcone derivatives as xanthine oxidase inhibitors.
Sichuan University
14
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
28
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
22
Discovery of new tetrahydroisoquinolines as potent and selective LSD1 inhibitors for the treatment of MLL-rearranged leukemia.
Zhejiang Ocean University
31
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Sun Yat-Sen University
30
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
33
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.
Zunyi Medical University
37
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
32
Design, synthesis, and biological evaluation of 3-phenyl substituted pyridine derivatives as potential dual inhibitors of XOR and URAT1.
South China University of Technology
25
Novel berberine derivatives as p300 histone acetyltransferase inhibitors in combination treatment for breast cancer.
Sichuan University
10
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
2
Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation.
Fudan University
3
Recent two-year advances in anti-dengue small-molecule inhibitors.
Macao University of Science and Technology
36
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.
Nankai University
27
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP.
Sun Yat-Sen University
54
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
3
Identification and in silicon binding study of a novel NR2B selective NMDAR antagonist.
Shenyang Pharmaceutical University
25
Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ inhibitors for hematological cancer.
Fudan University
1
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
25
Simplified staurosporine analogs as potent JAK3 inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
1
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
2
Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.
West China Hospital of Sichuan University
6
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
1
Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
The Affiliated Hospital of Southwest Medical University
1
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.
Chinese Academy of Sciences
10
Repurposing old drugs as novel inhibitors of human MIF from structural and functional analysis.
Wuhan University
70
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Wyeth Research
1
Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand.
Shanghai Institute of Traumatology and Orthopaedics
1
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
13
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Chinese Academy of Sciences
9
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
Sichuan University
20
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Chinese Academy of Sciences
3
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
1
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity.
Soochow University
10
Peptidylarginine deiminases 4 as a promising target in drug discovery.
Zhejiang Ocean University
75
Identification of Novel Fused Heteroaromatics-Based MALT1 Inhibitors by High-Throughput Screening to Treat B Cell Lymphoma.
Chinese Academy of Sciences
22
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.
Fudan University
9
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
27
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.
Fudan University
45
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
4
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of
Chinese Academy of Sciences
2
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
Nankai University
2
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
Nankai University
27
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Merck
38
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Merck Research Laboratories
6
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.
Huazhong University of Science & Technology
33
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
22
Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors.
Northwest A&F University
10
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
27
Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.
Tianjin University of Science and Technology
34
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
21
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Fudan University
45
Discovery of 3,3'-Spiro[Azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection.
Wuxi Apptec (Shanghai) Co.
1
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
23
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Merck
64
TGF-B INHIBITOR COMPOUND AND USE THEREOF
Medinno Pharmaceutical Technology (Zhuhai) Co.
319
CARBOXYLIC ACID-CONTAINING COMPOUNDS AS MODULATORS OF BIS-PHOSPHOGLYCERATE MUTASE FOR THE TREATMENT OF SICKLE CELL DISEASE
Genzyme
121
ATM kinase inhibitors and compositions and methods of use thereof
Chdi Foundation
10
INDOLE DERIVATIVES AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Mindset Pharma
5
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
71
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
127
Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity
Kancera
61
Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis
Pfizer
115
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
98
Substituted piperidine compounds and their use as orexin receptor modulators
Janssen Pharmaceutica
1
Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
Janssen Pharmaceutica
26
Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
10
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
32
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Glaxosmithkline