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题名: Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents
作者: Guo, Rui-Hua1, 2; Zhang, Quan1; Ma, Yun-Bao1; Luo, Jie1; Geng, Chang-An1, 2; Wang, Li-Jun1, 2; Zhang, Xue-Mei1; Zhou, Jun1; Jiang, Zhi-Yong1; null(陈纪军)1
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词: Anti-hepatitis B virus activity ; Quinolin-2(1H)-one ; Structure-activity relationships
英文摘要: A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC(50) = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC(50) = 0.026 mM, SI > 51) and the replication of HBV DNA (IC(50) = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II). Crown Copyright (C) 2010 Published by Elsevier Masson SAS. All rights reserved.
出版日期: 2011
卷号: 46, 期号:1, 页码:307-319
DOI标识: 10.1016/j.ejmech.2010.11.019
语种: 英语
ISSN号: 0223-5234
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/5385
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

Recommended Citation:
Guo, RH; Zhang, QA; Ma, YB; Luo, J; Geng, CA; Wang, LJ; Zhang, XM; Zhou, J; Jiang, ZY; Chen, JJ.Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(1):307-319
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