137 articles for Z Huang
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Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
Teva Branded Pharmaceutical Products R & D
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
Kbp Biosciences
Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.
Teva Branded Pharmaceutical Products R & D
Synthesis and Biological Evaluation of Novel Olean-28,13ß-lactams as Potential Antiprostate Cancer Agents.
China Pharmaceutical University
Transporter-mediated tissue targeting of therapeutic molecules in drug discovery.
Eli Lilly
Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors.
China Pharmaceutical University
Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.
China Pharmaceutical University
Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
Southeast University
NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity.
China Pharmaceutical University
A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.
Janssen Research and Development
Design, synthesis and evaluation of tacrine-flurbiprofen-nitrate trihybrids as novel anti-Alzheimer's disease agents.
China Pharmaceutical University
Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor.
State University of New York
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.
University of Alberta
2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.
Shanghai Jiao Tong University
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Cephalon
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Merck Frosst Centre For Therapeutic Research
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.
Cephalon
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.
Cephalon
Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.
Cephalon
Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies.
University of Alberta
Synthesis and biological evaluation of [D-lysine]8cyclosporin A analogs as potential anti-HCV agents.
Scynexis
Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.
Merck Frosst Center For Therapeutic Research
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Merck Frosst Centre For Therapeutic Research
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Merck Frosst Centre For Therapeutic Research
Naphthalenebis[alpha,alpha-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases.
University of Toronto
Synthesis and glutamate antagonist activity of 4-phosphonoalkylquinoline derivatives: A novel class of non-NMDA antagonist
TBA
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.
University of Alberta
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H3 receptor antagonists with potent cognition enhancing activity.
Cephalon
4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity.
Cephalon
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.
Cephalon
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
Merck Frosst Centre For Therapeutic Research
Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy.
Merck Frosst Centre For Therapeutic Research
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.
Cephalon
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
Merck Frosst Centre For Therapeutic Research
4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists.
Cephalon
Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.
Cephalon
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Cephalon
Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.
Merck Frosst Centre For Therapeutic Research
Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors.
University of Alberta
Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Merck Frosst Centre For Therapeutic Research
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Cephalon
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Merck Frosst Centre For Therapeutic Research
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.
University of Alberta
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Cephalon
2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.
Merck Frosst Centre For Therapeutic Research
Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.
Sepracor
Synthesis and biological evaluation of indomethacin analogs possessing a N-difluoromethyl-1,2-dihydropyrid-2-one ring system: a search for novel cyclooxygenase and lipoxygenase inhibitors.
University of Alberta
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Merck Frosst Centre For Therapeutic Research
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
University of Alberta
SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.
Scynexis
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
University of Alberta
SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Merck Frosst Centre For Therapeutic Research
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
University of Alberta
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
Merck Frosst Centre For Therapeutic Research
Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.
Institute For Medical Research
Thiazole analog as stearoyl-CoA desaturase 1 inhibitor.
Merck Frosst Centre For Therapeutic Research
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Merck Frosst Center For Therapeutic Research
Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.
Merck Frosst Center For Therapeutic Research
Development of Nitric Oxide-Donating Netarsudil Derivatives as a Synergistic Therapy for Glaucoma with Reduced Ocular Irritation.
China Pharmaceutical University
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
Johnson & Johnson Pharmaceutical Research and Development
Advances in nitric oxide regulators for the treatment of ischemic stroke.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus.
Sichuan University
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
Shanghai Institute of Materia Medica
Structure-Activity Relationship of Novel Pyrimidine Derivatives with Potent Inhibitory Activities against
Sichuan University
Discovery of potent human dihydroorotate dehydrogenase inhibitors based on a benzophenone scaffold.
Sichuan University
Novel neuroprotective pyromeconic acid derivatives with concurrent anti-Aβ deposition, anti-inflammatory, and anti-oxidation properties for treatment of Alzheimer's disease.
Fujian Medical University
HIV-1 gp120-CXCR4 recognition probed with synthetic nanomolar affinity D-peptides containing fragments of gp120 V3 loop.
Tsinghua University
Design, synthesis, and biological characterization of a new class of symmetrical polyamine-based small molecule CXCR4 antagonists.
Tsinghua University
Identification of the gossypol derivatives as androgen receptor inhibitor.
Zhejiang Normal University
A fragment integrational approach to GPCR inhibition: Identification of a high affinity small molecule CXCR4 antagonist.
Tsinghua University
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
Merck Frosst Center For Therapeutic Research
Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities.
Sun Yat-Sen University
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.
Sichuan University
A chemical strategy to promote helical peptide-protein interactions involved in apoptosis.
University of Illinois At Urbana-Champaign
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.
Nankai University
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
Wuxi Apptec
Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
Wuxi Apptec
Drug Repurposing of Quisinostat to Discover Novel
East China University of Science and Technology
Novel Bisubstrate Inhibitors for Protein N-Terminal Acetyltransferase D.
Purdue University
Synergetic inhibition of genistein and D-glucose on alpha-glucosidase.
Sun Yat-Sen (Zhongshan) University
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-
The Genomics Institute of The Novartis Research Foundation
Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors.
Peking University
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
Zhejiang University
Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
Shanghai Institute of Pharmaceutical Industry
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Merck Frosst Centre For Therapeutic Research
A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities.
Tsinghua University
Screening and biological evaluation of a novel STAT3 signaling pathway inhibitor against cancer.
Dalian Medical University
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.
Maternal and Child Health Hospital of Hubei Province
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Chinese Academy of Sciences
Efficacy and Tolerability of Pyrazolo[1,5-
The Genomics Institute of The Novartis Research Foundation
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Merck Frosst Centre For Therapeutic Research
Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.
Upstate Medical University
Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer.
China Pharmaceutical University
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis.
Nankai University
SAR study of celastrol analogs targeting Nur77-mediated inflammatory pathway.
Xiamen University
High affinity CXCR4 inhibitors generated by linking low affinity peptides.
University of California San Diego
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Chemical conversion of nicotinamide into type I positive allosteric modulator of α7 nAChRs.
Peking University
Substituted furans as inhibitors of the PDE4 enzyme.
Merck Frosst Centre For Therapeutic Research
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.
Nankai University
Identification and characterization of benzo[d]oxazol-2(3H)-one derivatives as the first potent and selective small-molecule inhibitors of chromodomain protein CDYL.
Peking University
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
Genentech
Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats.
The First Affiliated Hospital of Nanjing Medical University
Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
China Pharmaceutical University
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.
Peking University
Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.
China Pharmaceutical University
Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors.
State University of New York
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Eli Lilly
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
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
East China University of Science and Technology
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Novartis Institutes For Biomedical Research
Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.
National Center For Advancing Translational Sciences
Discovery of C-1 modified oseltamivir derivatives as potent influenza neuraminidase inhibitors.
Shandong University
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Shenyang Pharmaceutical University
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.
Nankai University
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Pfizer
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.
Nankai University
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.
Nankai University
Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy.
Crystal Pharmatech
Heterocyclic Compounds as Immunomodulators of PD-L1 Interactions
Ascletis Bioscience
Streptococcus mutans glucosyl transferase inhibitors for dental caries therapy
Uab Research Foundation
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International