175 articles for T Zhang
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Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.
Southern Medical University
Design, synthesis and bioactivity of novel phthalimide derivatives as acetylcholinesterase inhibitors.
Chinese Academy of Agricultural Sciences
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Merck Research Laboratories
Synthesis and evaluation of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives as non-purine xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Development of a novel class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Rapid development of two factor IXa inhibitors from hit to lead.
Merck Research Laboratories
Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening.
Astrazeneca
Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain.
Huazhong University of Science and Technology
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
Beijing Institute of Pharmacology & Toxicology
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Astrazeneca
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
Huazhong University of Science and Technology
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
University of Michigan
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
TBA
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Astrazeneca
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Harvard Medical School
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.
Harvard Medical School
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Abbott Laboratories
C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.
Harvard Medical School
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells.
Ocean University of China
Assessment of the structure-activity relationship and antileukemic activity of diacylpyramide compounds as human ClpP agonists.
University of Chinese Academy of Sciences
Tetrahydro-β-carboline derivatives as potent histone deacetylase 6 inhibitors with broad-spectrum antiproliferative activity.
Northwest A&F University
5-Cyano substituted diarylpyridines as potent HIV-1 NNRTIs: Rational design, synthesis, and activity evaluation.
Shandong University
Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC.
Puhe Biopharma
Discovery of novel substituted pyridine carboxamide derivatives as potent allosteric SHP2 inhibitors.
China Pharmaceutical University
Discovery of potent HIV-1 NNRTIs by CuAAC click-chemistry-based miniaturized synthesis, rapid screening and structure optimization.
Shandong University
Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).
Stanford University
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.
Zhejiang University
Structure-Guided Design, Synthesis, and Antivirulence Assessment of Covalent Staphylococcus aureus Sortase A Inhibitors.
Nanjing University of Chinese Medicine
Exploring the Function of (+)-Naltrexone Precursors: Their Activity as TLR4 Antagonists and Potential in Treating Morphine Addiction.
Chinese Academy of Sciences
ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases.
Stanford University
Discovery of novel deoxyvasicinone derivatives with benzenesulfonamide substituents as multifunctional agents against Alzheimer's disease.
Anhui Medical University
Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy.
Suzhou Genhouse Bio
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
BeiGene(Beiing) Co., Ltd.
Structure-Activity Relationship of Novel Pyrimidine Derivatives with Potent Inhibitory Activities against
Sichuan University
Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer.
East China Normal University
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions.
Dana-Farber Cancer Institute
Discovery of novel 2-hydroxyl-4-benzyloxybenzyl aniline derivatives as potential multifunctional agents for the treatment of Parkinson's disease.
North Sichuan Medical College
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Abbott Laboratories
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease.
Southern Medical University
In situ click chemistry-based discovery of 1,2,3-triazole-derived diarylpyrimidines as novel HIV-1 NNRTIs by exploiting the tolerant region I in binding pocket.
Shandong University
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Abbott Laboratories
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
Stanford University
Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
Beigene (Beijing) Co.
Recent advances in chemistry and bioactivity of marine cyanobacteria Moorea species.
Ningbo 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
Discovery of indole-piperazine derivatives as selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting activities and neuroprotective activities.
Northwest A&F University
Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs.
Shandong University
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Abbott Laboratories
Discovery of 4-methyl-3-(pyridin-2-ylamino)benzamide derivatives as C-Abl inhibitors with potential neuroprotective effect.
Southern Medical University
Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
Tianjin Institute of Medical & Pharmaceutical Sciences
Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis.
East China Normal University
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Jinan University
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.
Wenzhou Medical University
Intramolecular hydrogen bond interruption and scaffold hopping of TMC-5 led to 2-(4-alkoxy-3-cyanophenyl)pyrimidine-4/5-carboxylic acids and 6-(4-alkoxy-3-cyanophenyl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones as potent pyrimidine-based xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.
Pla Strategic Support Force Medical Center
Structure-Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors.
Chinese Academy of Sciences
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Stanford University
Therapeutic Activity of the Lansoprazole Metabolite 5-Hydroxy Lansoprazole Sulfide in Triple-Negative Breast Cancer by Inhibiting the Enoyl Reductase of Fatty Acid Synthase.
Indiana University School of Medicine
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.
Shanghaitech University
Synthesis of small molecules targeting paclitaxel-induced MyD88 expression in triple-negative breast cancer cell lines.
Universiti Kuala Lumpur
Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor.
Shanghai Hengrui Pharmaceutical
Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
Shenyang Pharmaceutical University
Elastase Inhibitor Cyclotheonellazole A: Total Synthesis and In Vivo Biological Evaluation for Acute Lung Injury.
Nankai University
Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.
China Pharmaceutical University
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis.
Shenyang Pharmaceutical University
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
Shandong University
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Harvard Medical School
Synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenylpyrimidine derivatives with 4-amino or 4-hydroxy as a pharmacophore element binding with xanthine oxidase active site.
Shenyang Pharmaceutical University
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
Shandong University
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.
Abbott Laboratories
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.
China Pharmaceutical University
Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
Shenyang Pharmaceutical University
Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma.
China Pharmaceutical University
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.
Shandong University
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.
Shanghai Hengrui Pharmaceutical
Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket.
Sun Yat-Sen University
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.
Chinese Academy of Sciences
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.
Lanzhou University
Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities.
China Pharmaceutical University
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.
Southern Medical University
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
Lanzhou University
Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.
St Louis College of Pharmacy and Washington University
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
China Pharmaceutical University
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ-Lyase.
Shanghai Jiao Tong University
Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.
Southern Medical University
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.
Dana-Farber Cancer Institute
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Institute of Organic Chemistry
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Harvard Medical School
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.
Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science & Technology)
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
Peking Union Medical College
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
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.
Chinese Academy of Sciences
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR
East China University of Science and Technology
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.
Sun Yat-Sen University
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
Peking Union Medical College
Bioactivatable Pseudotripeptidization of Cyclic Dipeptides To Increase the Affinity toward Oligopeptide Transporter 1 for Enhanced Oral Absorption: An Application to Cyclo(l-Hyp-l-Ser) (JBP485).
Dalian Medical University
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR
Jinan University
Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Harvard Medical School
Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors.
Southern Medical University
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Dana-Farber Cancer Institute
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.
Lanzhou University
Exploring the Natural Piericidins as Anti-Renal Cell Carcinoma Agents Targeting Peroxiredoxin 1.
Chinese Academy of Sciences
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.
Xi'An Jiaotong University
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
Xi'An Jiaotong University
Homo- and hetero-dimers of inactive organophosphorous group binding at dual sites of AChE.
Chinese Academy of Agricultural Sciences
Design, synthesis and biological evaluation of 1-hydroxy-2-phenyl-4-pyridyl-1H-imidazole derivatives as xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.
Beijing Institute of Pharmacology and Toxicology
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.
Shanghai University of Traditional Chinese Medicine
Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.
University of Kentucky
Discovery of tranylcypromine analogs with an acylhydrazone substituent as LSD1 inactivators: Design, synthesis and their biological evaluation.
Zhengzhou University
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.
Uit The Arctic University of Norway
Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors.
Southern Medical University
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
West China Hospital
Identification of Peptidic Antagonists of Vascular Endothelial Growth Factor Receptor 1 by Scanning the Binding Epitopes of Its Ligands.
Umr 8638 Cnrs
Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors.
Shanghai University of Traditional Chinese Medicine
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.
Mochida Pharmaceutical
NOVEL BENZOFURANYL HYDROXYPHENYL METHANONE DERIVATIVE COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
Innovo Therapeutics
Antimitotic amides for the treatment of cancer and proliferative disorders
Frost Biologic
PROTEASE INHIBITORS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
Merck Sharp & Dohme
Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as a Syk inhibitor
Kronos Bio
NITROGEN-CONTAINING HETEROCYCLIC POLYCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
Shanghai Hansoh Biomedical
Nitrogen-Containing Heterocyclic Compound, Pharmaceutical Compositions thereof and Use thereof
280 Bio
FUSED TETRACYCLIC QUINAZOLINE DERIVATIVES AS INHIBITORS OF ERBB2
Enliven Therapeutics
Substituted pyrrolo[2,3-d]pyrimidines and pyrazolo[3,4-d]pyrimidines as inhibitors for multi-resistant cancers
Ferris State University
Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein arginine methyl transferase 5 (PRMT5)
Prelude Therapeutics
Fused piperidinyl bicyclic and related compounds as modulators of C5A receptor
Inflarx
N4-hydroxycytidine and derivatives and anti-viral uses related thereto
Emory University
Piperidine derivatives as inhibitors of ubiquitin specific protease 7
Almac Discovery
Fluorescent antagonists of the A3 adenosine receptor
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
Albany Molecular Research
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Mcgill University
Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea.
Kitasato University