國家衛生研究院 NHRI:
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    日期题名關聯
    2022-11 Selective and antagonist-dependent µ-opioid receptor activation by the combination of 2-{[2-(6-chloro-3,4-dihydro-1(2H)-quinolinyl)-2-oxoethyl]sulfanyl}-5-phenyl-4,6-(1H,5H)-pyrimidinedione and naloxone/naltrexone Bioorganic Chemistry. 2022 Nov;128:Article number 105905.
    2021-08-01 DBPR108, a novel dipeptidyl peptidase-4 inhibitor with antihyperglycemic activity Life Sciences. 2021 Aug 1;278:Article number 119574.
    2021-01 BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy Translational Oncology. 2021 Jan;14(1):Article number 100897.
    2019-04-01 A novel, potent, and orally bioavailable thiazole HCV NS5A inhibitor for the treatment of hepatitis C virus European Journal of Medicinal Chemistry. 2019 Apr 1;167:245-268.
    2019-04-01 The in vivo antinociceptive and mu-opioid receptor activating effects of the combination of N-phenyl-2′,4′-dimethyl-4,5′-bi-1,3-thiazol-2-amines and naloxone European Journal of Medicinal Chemistry. 2019 Apr 1;167:312-323.
    2019-03 Synthesis and biological evaluation of N-glucosyl indole derivatives as sodium-dependent glucose co-transporter 2 inhibitors Bioorganic Chemistry. 2019 Mar;83:520-525.
    2018-04 4-Bromophenylhydrazinyl benzenesulfonylphenylureas as indoleamine 2,3-dioxygenase inhibitors with in vivo target inhibition and anti-tumor efficacy Bioorganic Chemistry. 2018 Apr;77:600-607.
    2018-01-01 Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2 European Journal of Medicinal Chemistry. 2018 Jan 1;143:611-620.
    2017-06-22 Targeting coronaviral replication and cellular JAK2 mediated dominant NF-kappaB activation for comprehensive and ultimate inhibition of coronaviral activity Scientific Reports. 2017 Jun 22;7:Article number 4105.
    2017-01 A potent, selective, and orally bioavailable HCV NS5A inhibitor for treatment of Hepatitis C Virus: (S)-1-((R)-2-(Cyclopropanecarboxamido)-2-phenylacetyl)-N-(4-phenylthiazo l-2-yl)pyrrolidine-2-carboxamide Journal of Medicinal Chemistry. 2017 Jan;60(1):228-247.
    2016-05 N-Indolylglycosides bearing modifications at the glucose C6-Position as Sodium-Dependent Glucose Co-transporter 2 inhibitors Bioorganic and Medicinal Chemistry. 2016 May;24(10):2242-2250.
    2016-01 Phenyl benzenesulfonylhydrazides exhibit selective Indoleamine 2,3-Dioxygenase inhibition with potent in vivo pharmacodynamic activity and antitumor efficacy Journal of Medicinal Chemistry. 2016 Jan;59(1):419-430.
    2015-07 Development and application of a fluorescent glucose uptake assay for the high-throughput screening of non-glycoside SGLT2 inhibitors European Journal of Pharmaceutical Sciences. 2015 Jul;74:40-44.
    2015-07 Pharmacological induction of human fetal globin gene in hydroxyurea-resistant primary adult erythroid cells Molecular and Cellular Biology. 2015 Jul;35(14):2541-2553.
    2015-07 Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations European Journal of Medicinal Chemistry. 2015 Jul;100:151-161.
    2015-05 A novel peripheral cannabinoid receptor 1 antagonist, BPR0912, reduces weight independently of food intake and modulates thermogenesis Diabetes, Obesity and Metabolism. 2015 May;17(5):495-504.
    2014-12-01 Morphine drives internal ribosome entry site-mediated hnRNP K translation in neurons through opioid receptor-dependent signaling Nucleic Acids Research. 2014 Dec 1;42(21):13012-13025.
    2014-09 Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists Bioorganic and Medicinal Chemistry. 2014 Sep;22(17): 4694-4703.
    2014-08 Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors Bioorganic and Medicinal Chemistry Letters. 2014 Aug;24(15):3403-3406.
    2014-08 Discovery of selective inhibitors of Glutaminase-2, which inhibit mTORC1, activate autophagy and inhibit proliferation in cancer cells Oncotarget. 2014 Aug;5(15):6087-6101.
    2014-01-08 Evaluation of the antitumor effects of BPR1J-340, a potent and selective FLT3 inhibitor, alone or in combination with an HDAC inhibitor, vorinostat, in AML cancer PLoS ONE. 2014 Jan 8;9(1):Article number e83160.
    2013-11-13 Discovery of 1-(2,4-Dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5 -(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice Journal of Medicinal Chemistry. 2013 Nov 13;56(24):9920-9933.
    2013-11 BPR0C305, an orally active microtubule-disrupting anticancer agent Anticancer Drugs. 2013 Nov;24(10):1047-1057.
    2013-06-28 Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine aurora kinase inhibitor Journal of Medicinal Chemistry. 2013 Jun 28;56(13):5247-5260.
    2013-06 c-Jun-mediated anti-cancer mechanisms of tylophorine Carcinogenesis. 2013 Jun;34(6):1304-1314.
    2013-06 Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) Bioorganic and Medicinal Chemistry. 2013 Jun;21(11):2856-2867.
    2013-05 Characterization of an efficient dengue virus replicon for development of assays of discovery of small molecules against dengue virus Antiviral Research. 2013 May;98(2):228-241.
    2013-05 Aurora kinase inhibitors reveal mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules Proceedings of the National Academy of Sciences of the United States of America. 2013 May;110(19):E1779-E1787.
    2013-05 Protein kinase inhibitor design by targeting the Asp-Phe-Gly (DFG) motif: The role of the DFG motif in the design of epidermal growth factor receptor inhibitors Journal of Medicinal Chemistry. 2013 May;56(10):3889-3903.
    2013-02 Resistance studies of a di-thiazol analogue, DBPR110, as a potential hepatitis C virus NS5A inhibitor in replicon systems Antimicrobial Agents and Chemotherapy. 2013 Feb; 57(2):723-733.
    2013-01 3D-QSAR-assisted drug design: Identification of a potent quinazoline-based aurora kinase inhibitor ChemMedChem. 2013 Jan;8(1):136-148.
    2012-12-13 Synthesis and biological evaluation of tylophorine-derived dibenzoquinolines as orally active agents: Exploration of the role of tylophorine e ring on biological activity Journal of Medicinal Chemistry. 2012 Dec 13;55(23):10363-10377.
    2012-12 An efficient, mild and scalable synthesis of bioactive compounds containing the angelicin scaffold Journal of the Chinese Chemical Society. 2012 Dec;59(12):1548-1554.
    2012-09 Anti-influenza drug discovery: Identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization ChemMedChem. 2012 Sep;7(9):1546-1550.
    2012-09 Putative tumor metastasis-associated genes in human gastric cancer International Journal of Oncology. 2012 Sep;41(3):1068-1084.
    2012-07 Induction of fatty acid oxidation resists weight gain, ameliorates hepatic steatosis and reduces cardiometabolic risk factors International Journal of Obesity. 2012 Jul;36(7):999-1006.
    2012-06-07 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) Bioorganic and Medicinal Chemistry Letters. 2012 Jun 7;22(14):4654-4659.
    2012-06 EGFR and myosin II inhibitors cooperate to suppress EGFR-T790M-mutant NSCLC cells Molecular Oncology. 2012 Jun;6(3):299-310.
    2012-02 Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents Investigational New Drugs. 2012 Feb;30(1):164-175.
    2012-02 Discovery of novel stem cell mobilizers that target the CXCR4 receptor ChemMedChem. 2012 Feb;7(2):209-212.
    2012-01 Resistance analysis and characterization of a thiazole analogue, BP008, as a potent hepatitis C virus NS5A inhibitor Antimicrobial Agents and Chemotherapy. 2012 Jan;56(1):44-53.
    2012-01 BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML British Journal of Cancer. 2012 Jan;106(3):475-481.
    2012-01 A High-throughput cell-based screening for L858R/T790M mutant epidermal growth factor receptor inhibitors Anticancer Research. 2012 Jan;32(1):147-151.
    2011-11 Isolation and biological activities of phenanthroindolizidine and septicine alkaloids from the formosan tylophora ovata Planta Medica. 2011 Nov;77(17):1932-1938.
    2011-09 Inhibition of HIV-1 Tat-mediated transcription by a coumarin derivative, BPRHIV001, through the Akt pathway Journal of Virology. 2011 Sep;85(17):9114-9126
    2011-07-25 The first total synthesis of cytopiloyne, an anti-diabetic, polyacetylenic glucoside Chemistry-A European Journal. 2011 Jul 25;17(31):8696-8703.
    2011-07 Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) Bioorganic and Medicinal Chemistry. 2011 Jul;19(14):4173-4182 .
    2011-06 Hot topic: Opportunities and potential challenges for the treatment of metabolic syndrome Current Topics In Medicinal Chemistry. 2011 Jun;11(12):1420.
    2011-04 Isatin-beta-thiosemicarbazones as potent herpes simplex virus inhibitors Bioorganic and Medicinal Chemistry Letters. 2011 Apr;21(7):1948-1952.
    2011-03 Successful propagation of flavivirus infectious cDNAs by a novel method to reduce the cryptic bacterial promoter activity of virus genomes Journal of Virology. 2011 Mar;85(6):2927-2941.

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