國家衛生研究院 NHRI:
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    近3年内发表的文件:1(2.17%)
    含全文笔数:46(100.00%)

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    显示项目1-46 / 46. (共1页)
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    日期题名關聯
    2022-02-05 Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design European Journal of Medicinal Chemistry. 2022 Feb 5;229:Article number 114043.
    2021-08-12 Xanthine derivatives reveal an allosteric binding site in methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) Journal of Medicinal Chemistry. 2021 Aug 12;64(15):11288-11301.
    2020-02-10 Unique sulfur-aromatic interactions contribute to the binding of potent imidazothiazole indoleamine 2,3-Dioxygenase inhibitors Journal of Medicinal Chemistry. 2020 Feb 10;63(4):1642-1659.
    2019-12 Identification of a multitargeted tyrosine kinase inhibitor for the treatment of gastrointestinal stromal tumors and acute myeloid leukemia Journal of Medicinal Chemistry. 2019 Dec;62(24):11135-11150.
    2019-11-27 Discovery of a furanopyrimidine-based epidermal growth factor receptor inhibitor (DBPR112) as a clinical candidate for the treatment of non-small cell lung cancer Journal of Medicinal Chemistry. 2019 Nov 27;62(22):10108-10123.
    2019-04-10 Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants Journal of Medicinal Chemistry. 2019 Apr 10;62(8):3940-3957.
    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.
    2017-06 Mutagenesis of dengue virus protein NS2A revealed a novel domain responsible for virus-induced cytopathic effect and interactions between NS2A and NS2B transmembrane segments Journal of Virology. 2017 Jun;91(12):Article number e01836-16.
    2016-04-12 Pyrazolylamine derivatives reveal the conformational switching between type I and type II binding modes of Anaplastic Lymphoma Kinase (ALK) Journal of Medicinal Chemistry. 2016 Apr 12;59(8):3906-3919.
    2016-01 Important hydrogen bond networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) inhibitor design revealed by crystal structures of imidazoleisoindole derivatives with IDO1 Journal of Medicinal Chemistry. 2016 Jan;59 (1):282-293.
    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.
    2015-10 Identification of substituted naphthotriazolediones as novel tryptophan 2,3-dioxygenase (TDO) inhibitors through structure-based virtual screening Journal of Medicinal Chemistry. 2015 Oct;58 (19):7807-7819.
    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.
    2013-09 Furanylazaindoles: Potent anticancer agents in vitro and in vivo Journal of Medicinal Chemistry. 2013 Sep;56(20):8008-8018.
    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.
    2012-08 Development of an anti-influenza drug screening assay targeting nucleoproteins with tryptophan fluorescence quenching Analytical Chemistry. 2012 Aug;84(15):6391-6399.
    2012-02 Discovery of novel stem cell mobilizers that target the CXCR4 receptor ChemMedChem. 2012 Feb;7(2):209-212.
    2011-09 Synthesis and biological evaluation of 1-(4′-Indolyl and 6′-Quinolinyl) indoles as a new class of potent anticancer agents European Journal of Medicinal Chemistry. 2011 Sep;46(9):3623-3629.
    2011-04-28 Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-Fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents Journal of Medicinal Chemistry. 2011 Apr 28;54(8):3076-3080.
    2010-12 Discovery of non-glycoside sodium-dependent glucose Co-transporter 2 (SGLT2) inhibitors by ligand-based virtual screening Journal of Medicinal Chemistry. 2010 Dec;53(24):8770-8774.
    2010-10 Structural basis for the improved potency of peroxisome proliferator-activated receptor (PPAR) agonists ChemMedChem. 2010 Oct;5(10):1707-1716.
    2010-09 Cancer cells acquire mitotic drug resistance properties through beta i-tubulin mutations and alterations in the expression of beta-tubulin isotypes PLoS ONE. 2010 Sep;5(9):Article number e12564.
    2010-06-15 Fast-forwarding hit to lead: Aurora and epidermal growth factor receptor kinase inhibitor lead identification Journal of Medicinal Chemistry. 2010 Jun 15;53(13):4980-4988.
    2010-03-11 5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors Journal of Medicinal Chemistry. 2010 Mar 11;53(5):2309-2313.
    2010-02-01 Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor ChemMedChem. 2010 Feb 1;5(2):255-267.
    2009-10 (1,3-Diphenyl-1H-pyrazol-4-yl)-methylamine analogues as inhibitors of dipeptidyl peptidases Journal of the Chinese Chemical Society. 2009 Oct;56(5):1048-1055.
    2009-08-13 Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach Journal of Medicinal Chemistry. 2009 Aug 13;52(15):4941-4945.
    2009-07-23 Generation of ligand-based pharmacophore model and virtual screening for identification of novel tubulin inhibitors with potent anticancer activity Journal of Medicinal Chemistry. 2009 Jul 23;52(14):4221-4233.
    2009-06 A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitiors [Erratum: European Journal of Medicinal Chemistry. 2008 Aug;43(8):1603-1611.] European Journal of Medicinal Chemistry. 2009 Jun;44(6):2763-2763.
    2009-04-23 Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists Journal of Medicinal Chemistry. 2009 Apr 23;52(8):2618-2622.
    2009-02-26 Structure-based drug design of novel aurora kinase a inhibitors: Structural basis for potency and specificity Journal of Medicinal Chemistry. 2009 Feb 26;52(4):1050-1062.
    2008-12-25 Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents Journal of Medicinal Chemistry. 2008 Dec 25;51(24):8163-8167.
    2008-08 A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors European Journal of Medicinal Chemistry. 2008 Aug;43(8):1603-1611.
    2008-03-01 Aurora kinase A inhibitors: Identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold Bioorganic and Medicinal Chemistry Letters. 2008 Mar;18(5):1623-1627.
    2008 Structure-based inhibitors exhibit differential activities against Helicobacter pylori and Escherichia coli undecaprenyl pyrophosphate synthases Journal of Biomedicine and Biotechnology. 2008; 2008:Article number 841312.
    2006-10-19 Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists Journal of Medicinal Chemistry. 2006 Oct;49(21):6421-6424.
    2006-08-24 Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease Journal of Medicinal Chemistry. 2006 Aug;49(17):5154-5161.
    2006-06-15 Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies Journal of Medicinal Chemistry. 2006 Jun;49(12):3485-3495.
    2006-05-04 Structure-based drug design of a novel family of PPAR gamma partial agonists: Virtual screening, X-ray crystallography, and in vitro/in vivo biological activities Journal of Medicinal Chemistry. 2006 May;49(9):2703-2712.
    2006-02-09 Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: Design, synthesis, structural biology, and molecular docking studies Journal of Medicinal Chemistry. 2006 Feb;49(3):1212-1216.
    2006-01-12 2-[3-[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV Journal of Medicinal Chemistry. 2006 Jan;49(1):373-380.
    2005-12-29 Novel indole-based peroxisome proliferator-activated receptor agonists: Design, SAR, structural biology, and biological activities Journal of Medicinal Chemistry. 2005 Dec;48(26):8194-8208.
    2005-12-15 The effect of N-terminal truncation on double-dimer assembly of goose delta-crystallin Biochemical Journal. 2005 Dec;392(Pt. 3):545-554.
    2005-07-01 Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors Bioorganic and Medicinal Chemistry Letters. 2005 Jul;15(13):3271-3275.

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