147 articles for Z Zhao
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Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
High Magnetic Field Laboratory
Substituted 4-morpholine N-arylsulfonamides as¿-secretase inhibitors.
Merck Research Laboratories
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.
East China University of Science and Technology
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Merck Research Laboratories
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Chinese Academy of Sciences
Synthesis and optimization of N-heterocyclic pyridinones as catechol-O-methyltransferase (COMT) inhibitors.
Merck
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.
High Magnetic Field Laboratory
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.
Genentech
Discovery of a Novel, Potent Spirocyclic Series of¿-Secretase Inhibitors.
Merck Research Laboratories
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor.
East China Normal University
Synthesis and Evaluation of Heterocyclic Catechol Mimics as Inhibitors of Catechol-O-methyltransferase (COMT).
Merck Research Laboratories
Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.
University of Maryland
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.
East China University of Science and Techology
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5.
University of Maryland
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
Genentech
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Gilead Sciences
Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening.
East China University of Science and Technology
Novel nonsecosteroidal VDR agonists with phenyl-pyrrolyl pentane skeleton.
China Pharmaceutical University
Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives.
State Key Laboratory of Bioreactor Engineering
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
East China University of Science and Technology
Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship.
East China University of Science and Technology
Discovery of diverse human dihydroorotate dehydrogenase inhibitors as immunosuppressive agents by structure-based virtual screening.
State Key Laboratory of Bioreactor Engineering
X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.
Sanofi Us
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
Amgen
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Merck
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Emd-Serono Research Institute
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Emd-Serono Research Institute
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
Emd-Serono Research Institute
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Merck
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Pfizer
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Merck And
Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase.
Pfizer
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious¿-secretase modulators in vivo.
Schering-Plough Research Institute
Discovery of novel selective inhibitors for EGFR-T790M/L858R.
Dalian University of Technology
SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration.
East China University of Science and Technology
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Merck Research Laboratories
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Merck Research Laboratories
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Merck Research Laboratories
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Merck
Discovery of 3-(1H-benzo[d]imidazole-2-yl)-1H-pyrazol-4 -amine derivatives as novel and potent syk inhibitors for the treatment of hematological malignancies.
China Pharmaceutical University
Discovery of benzofuran-2-carboxylic acid derivatives as lymphoid tyrosine phosphatase (LYP) inhibitors for cancer immunotherapy.
Shandong University
Design, synthesis and bioactivity evaluation of isobavachin derivatives as hURAT1 inhibitors for hyperuricemia agents.
Southern Medical University
Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives.
China Pharmaceutical University
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
Schering-Plough Research Institute
Development of Degraders of Cyclin-Dependent Kinases 4 and 6 Based on Rational Drug Design.
East China Normal University
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Schering-Plough Research Institute
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.
Schering-Plough Research Institute
Discovery and Characterization of Moracin C as an Anti-Gouty Arthritis/Hyperuricemia Candidate by Docking-Based Virtual Screening and Pharmacological Evaluation.
Southern Medical University
Medicinal Chemistry Insights into the Development of Small-Molecule Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.
China Pharmaceutical University
Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.
Southern Medical University
Review of bioactivity and structure-activity relationship on baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone) derivatives: Structural modifications inspired from flavonoids in Scutellaria baicalensis.
Shaanxi University of Chinese Medicine
Discovery of 2,4-diphenyl-substituted thiazole derivatives as PRMT1 inhibitors and investigation of their anti-cervical cancer effects.
Minzu University of China
Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance.
Southeast University
Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.
East China University of Science and Technology
Discovery of aromatic 2-(3-(methylcarbamoyl) guanidino)-N-aylacetamides as highly potent chitinase inhibitors.
China Agricultural University
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.
Northwest University
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Merck
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.
East China University of Science & Technology
Discovery of novel verinurad analogs as dual inhibitors of URAT1 and GLUT9 with improved Druggability for the treatment of hyperuricemia.
Southern Medical University
Mechanism of Action and Structure-Activity Relationship of α-Conotoxin Mr1.1 at the Human α9α10 Nicotinic Acetylcholine Receptor.
Ocean University of China
Discovery of Cyclic Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy.
University of Missouri-Kansas City
Research progress in biological activities of isochroman derivatives.
Shaanxi University of Chinese Medicine
Meroterpenoids produced by fungi: Occurrence, structural diversity, biological activities, and their molecular targets.
Guangzhou University of Chinese Medicine
Discovery, Optimization, and Structure-Activity Relationship Study of Novel and Potent RSK4 Inhibitors as Promising Agents for the Treatment of Esophageal Squamous Cell Carcinoma.
East China University of Science & Technology
Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
Berlex Biosciences
Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
Berlex Biosciences
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.
Berlex Biosciences
Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists.
China Pharmaceutical University
Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
Shandong University
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.
East China University of Science & Technology
Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation.
East China University of Science & Technology
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Gilead Sciences
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.
East China University of Science and Technology
Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants.
East China University of Science & Technology
Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors.
Merck Research Laboratories
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
University of Connecticut
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
Berlex Biosciences
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.
Berlex Biosciences
Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.
East China University of Science and Technology
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR
East China University of Science and Technology
Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.
East China University of Science & Technology
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
Northwest University
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.
East China University of Science & Technology
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
Homoisoflavonoids as potential imaging agents for β-amyloid plaques in Alzheimer's disease.
Hefei University of Technology
Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.
East China University of Science & Technology
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Merck Research Laboratory
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.
Merck Research Laboratories
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Merck
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Schering-Plough Research Institute
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Schering-Plough Research Institute
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Schering-Plough Research Institute
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
Wuhan University
Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.
Merck Research Laboratories
Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.
East China University of Science and Technology
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Genentech
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.
Second Military Medical University
Isoquinolinone compound for inhibiting ssao/vap-1, and use thereof
Sunshine Lake Pharma Co.
CRYSTAL FORM AND SALT FORM OF BROMINE DOMAIN PROTEIN INHIBITOR AND PREPARATION METHOD THEREFOR
Chia Tai Tianqing Pharmaceutical Group
(4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
Genentech
Benzene disulfonamide for the treatment of cancer
Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften
Pyrimido[5,4-B]indolizine or pyrimido[5,4-B]pyrrolizine compound, preparation method and use thereof
Shanghai Institute of Materia Medica, Chinese Acad
RIP1 inhibitory compounds and methods for making and using the same
Rigel Pharmaceuticals
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
Janssen Pharmaceutica
Compounds inhibiting eukaryotic elongation factor 2 kinase activity
Longevica Pharmaceuticals
Dihalogenated sulfanilamides and benzolamides are effective inhibitors of the three ß-class carbonic anhydrases from Mycobacterium tuberculosis.
Universit�� Degli Studi Di Firenze
Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity.
Agri Ibrahim Cecen University
Glutathione transferase from Plasmodium falciparum--interaction with malagashanine and selected plant natural products.
University of Zimbabwe
Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
Senhwa Biosciences
Alicyclic[c] benzopyrone derivatives and uses thereof
Huazhong University of Science & Technology
5-membered ring heteroaromatic derivatives having NPY Y5 receptor antagonistic activity
Shionogi
Farnesyl diphosphate synthase inhibitors from in silico screening.
University of California San Diego
Synthesis of a diverse library of mechanism-based cysteine protease inhibitors.
University of California Berkeley
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.
University of Zimbabwe
Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line.
Brigham and Women'S Hospital
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Merck Research Laboratories