138 articles for F Wang
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Discovery of novel CDK8 inhibitors using multiple crystal structures in docking-based virtual screening.
West China Hospital of Sichuan University
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Genentech
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Pfizer
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
West China Hospital of Sichuan University
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Ariad Pharmaceuticals
Molecular design, synthesis and anticoagulant activity evaluation of fluorinated dabigatran analogues.
Shanghai Institute of Technology
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
Sichuan University
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
The interaction of 4-thiazolidinone derivatives containing indolin-2-one moiety with P-glycoprotein studied using K562 cell lines.
The First Affiliated Hospital of Dalian Medical University
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
Xuanzhu Pharma
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.
Jiangsu Aosaikang Pharmaceutical
Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.
Xi'An Jiaotong University
Synthesis, characterization, screening and docking analysis of 4-anilinoquinazoline derivatives as tyrosine kinase inhibitors.
Chinese Academy of Sciences
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
The Beatson Institute For Cancer Research
M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.
Glaxosmithkline
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.
Glaxosmithkline
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Design, synthesis, biochemical studies, cellular characterization, and structure-based computational studies of small molecules targeting the urokinase receptor.
Indiana University
Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity,ß-amyloid aggregation and Ca²¿ overload.
Huazhong University of Science and Technology
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.
Zhejiang Betapharma
Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases.
Huazhong University of Science and Technology
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
The Beatson Institute For Cancer Research
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyr
Pfizer
Photoregulation of thrombin aptamer activity using Bhc caging strategy.
University of Science and Technology of China
Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity.
Chinese Academy of Sciences
mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).
Sepracor
Design, synthesis, and examination of neuron protective properties of alkenylated and amidated dehydro-silybin derivatives.
Pharmacy School of Wenzhou Medical College
Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay.
The Second Military Medical University
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.
Beijing National Laboratory For Molecular Sciences
Virtual screening targeting the urokinase receptor, biochemical and cell-based studies, synthesis, pharmacokinetic characterization, and effect on breast tumor metastasis.
Indiana University School of Medicine
Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.
Sunovion Pharmaceuticals
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid.
Texas A&M University
Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.
Sunovion Pharmaceuticals
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Sepracor
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
Ariad Pharmaceuticals
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
Pharmacy School of Wenzhou Medical College
Dual integrin and gastrin-releasing peptide receptor targeted tumor imaging using 18F-labeled PEGylated RGD-bombesin heterodimer 18F-FB-PEG3-Glu-RGD-BBN.
Stanford University School of Medicine
Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.
Glaxosmithkline
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Ariad Pharmaceuticals
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Glaxosmithkline
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
ARIAD Pharmaceuticals, Inc.
Discovery of highly potent covalent SARS-CoV-2 3CLpro inhibitors bearing 2-sulfoxyl-1,3,4-oxadiazole scaffold for combating COVID-19.
Shanghai University of Traditional Chinese Medicine
Development of novel celastrol-ligustrazine hybrids as potent peroxiredoxin 1 inhibitors against lung cancer.
Anhui University of Science and Technology
Current therapy in amyotrophic lateral sclerosis (ALS): A review on past and future therapeutic strategies.
Nanjing University of Chinese Medicine
Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis.
Chinese Academy of Sciences
Discovery of novel CXCR4 inhibitors for the treatment of inflammation by virtual screening and biological evaluation.
Anhui Medical University
Discovery of novel deoxyvasicinone derivatives with benzenesulfonamide substituents as multifunctional agents against Alzheimer's disease.
Anhui Medical University
Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Insilico Medicine Shanghai Ltd
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.
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis.
China Pharmaceutical University
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
Discovery of benzodiazepine derivatives as a new class of covalent inhibitors of SARS-CoV-2 main protease.
Sichuan University
Optimization of 1,2,4-Triazole-Based p97 Inhibitors for the Treatment of Cancer.
University of Pittsburgh Chemical Diversity Center
Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors.
Shenyang Pharmaceutical University
Identification of (S)-1-(2-(2,4-difluorophenyl)-4-oxothiazolidin-3-yl)-3-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)urea as a potential anti-colorectal cancer agent.
Zunyi Medical University
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex.
University of Toronto
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 the design and discovery of synthetic tyrosinase inhibitors.
National Clinical Research Center For Geriatrics
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.
Shandong First Medical University and Shandong Academy of Medical Sciences
A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism.
Shanghai University of Traditional Chinese Medicine
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.
University of Kansas
Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.
Sichuan University
Discovery of 9,10-dihydrophenanthrene derivatives as SARS-CoV-2 3CL
Shanghai University of Traditional Chinese Medicine
Discovery of small-molecule inhibitors of RUVBL1/2 ATPase.
California Institute of Technology
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.
Chinese Academy of Sciences
Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis.
Sichuan University
Dual target inhibitors based on EGFR: Promising anticancer agents for the treatment of cancers (2017-).
Zhuhai Campus of Zunyi Medical University
Discovery of corticotropin releasing factor 2 receptor selective sauvagine analogues for treatment of skeletal muscle atrophy.
Procter & Gamble Pharmaceuticals
Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
Guizhou Medical University
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6
Sichuan University
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.
Shanghai University of Traditional Chinese Medicine
A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cells.
California Institute of Technology
Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer.
Zhuhai Campus of Zunyi Medical University
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
TBA
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Jiangsu Aosaikang Pharmaceutical
Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.
Lilly China Research and Development Center (Lcrdc)
Identification of human lactate dehydrogenase A inhibitors with anti-osteosarcoma activity through cell-based phenotypic screening.
Jilin University China-Japan Union Hospital
Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design.
Vanderbilt University
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.
Jiangsu Aosaikang Pharmaceutical
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.
Vanderbilt University
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
TBA
Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy.
TBA
Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery.
Dalian University of Technology
Design of N-Benzoxaborole Benzofuran GSK8175-Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV Inhibitor.
Glaxosmithkline
Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.
Nankai University
DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors.
Glaxosmithkline
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Agios Pharmaceuticals
Multistage virtual screening and identification of novel HIV-1 protease inhibitors by integrating SVM, shape, pharmacophore and docking methods.
Nankai University
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
Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors.
Fudan University
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Astrazeneca
Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone.
Pfizer
Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.
TBA
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Agios Pharmaceuticals
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.
Pfizer
Discovery of imidazoleisoindole derivatives as potent IDO1 inhibitors: Design, synthesis, biological evaluation and computational studies.
China Pharmaceutical University
Discovery of potent IDO1 inhibitors derived from tryptophan using scaffold-hopping and structure-based design approaches.
China Pharmaceutical University
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Wuxi Apptec
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2.
Guizhou Medical University
Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.
Progenra
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Genentech
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.
West China Hospital of Sichuan University
Picomolar inhibition ofβ-galactosidase (bovine liver) attributed to loop closure.
University of Arkansas
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Sichuan University and Collaborative Innovation Center
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Genentech
Quinoxaline compounds as type III receptor tyrosine kinase inhibitors
Development Center For Biotechnology
Nitrogen-containing tricyclic derivatives having HIV replication inhibitory activity
Shionogi
1-(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido [2, 3-B]pyrazin- 8-yl)oxy]phenyl]urea derivatives as RAF inhibitors for the treatment of cancer
Cancer Research Technology
Perfluoro-tert-butyl Homoserine Is a Helix-Promoting, Highly Fluorinated, NMR-Sensitive Aliphatic Amino Acid: Detection of the Estrogen Receptor·Coactivator Protein-Protein Interaction by (19)F NMR.
University of Delaware
Bivalent inhibitors of IAP proteins and therapeutic methods using the same
University of Michigan