國家衛生研究院 NHRI:Item 3990099045/3745
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/3745


    Title: Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors
    Other Titles: Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline1-carbothioic acid amide derivatives as novel HCV inhibitors
    Authors: Kang, IJ;Wang, LW;Hsu, SJ;Lee, CC;Lee, YC;Wu, YS;Hsu, TA;Yueh, A;Chao, YS;Chern, JH
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: An efficient synthetic methodology to provide indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives is described. These conformationally restricted heterobicyclic scaffolds were evaluated as a novel class of HCV inhibitors. Introduction of an acyl group at the NH2 of the thiourea moiety has been found to enhance inhibitory activity. The chain length and the position of the alkyl group on the indoline aromatic ring markedly influenced anti-HCV activity. The indoline scaffold was more potent than the corresponding indole and tetrahydroquinoline scaffolds and analogue 31 displayed excellent activity (EC50 = 510 nM) against HCV without significant cytotoxicity (CC50 >50 μM).
    Date: 2009-08-01
    Relation: Bioorganic and Medicinal Chemistry Letters. 2009 Aug 1;19(15):4134-4138.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2009.06.009
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000267900900030
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=67650164756
    Appears in Collections:[Jyh-Haur Chern] Periodical Articles
    [Yu-Sheng Chao(2002-2013)] Periodical Articles
    [Yueh Andrew Yueh] Periodical Articles
    [John Tsu-An Hsu] Periodical Articles

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