國家衛生研究院 NHRI:Item 3990099045/3745
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    题名: Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors
    其它题名: Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline1-carbothioic acid amide derivatives as novel HCV inhibitors
    作者: Kang, IJ;Wang, LW;Hsu, SJ;Lee, CC;Lee, YC;Wu, YS;Hsu, TA;Yueh, A;Chao, YS;Chern, JH
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: 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).
    日期: 2009-08-01
    關聯: 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
    显示于类别:[陳志豪] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [岳嶽] 期刊論文
    [徐祖安] 期刊論文

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