國家衛生研究院 NHRI:Item 3990099045/5014
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    题名: Synthesis, activity, and pharmacokinetic properties of a series of conformationally-restricted thiourea analogs as novel hepatitis C virus inhibitors
    作者: Kang, IJ;Wang, LW;Yeh, TK;Lee, CC;Lee, YC;Hsu, SJ;Wu, YS;Wang, JC;Chao, YS;Yueh, A;Chern, JH
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: A series of novel conformationally-restricted thiourea analogs were designed, synthesized, and evaluated for their anti-HCV activity. Herein we report the synthesis, structure–activity relationships (SARs), and pharmacokinetic properties of this new class of thiourea compounds that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay. Among compounds tested, the fluorene compound 4b was found to possess the most potent activity (EC50 = 0.3 μM), lower cytotoxicity (CC50 > 50 μM), and significantly better pharmacokinetic properties compared to its corresponding fluorenone compound 4c.
    日期: 2010-09-01
    關聯: Bioorganic and Medicinal Chemistry. 2010 Sep ;18(17):6414-6421.
    Link to: http://dx.doi.org/10.1016/j.bmc.2010.07.002
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000281203300023
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77955982883
    显示于类别:[趙宇生(2002-2013)] 期刊論文
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    [岳嶽] 期刊論文
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