| 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 | |
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; Chen, Ji-Jun1
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| 通讯作者 | Chen, JJ (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China |
| 2011 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| ISSN | 0223-5234 |
| 卷号 | 46期号:1页码:307-319 |
| 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. |
| 关键词 | Anti-hepatitis b Virus Activity Quinolin-2(1h)-one Structure-activity Relationships |
| 学科领域 | Pharmacology & Pharmacy |
| DOI | 10.1016/j.ejmech.2010.11.019 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000286905400036 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/5385 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 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 |
| 推荐引用方式 GB/T 7714 | Guo, Rui-Hua,Zhang, Quan,Ma, Yun-Bao,et al. 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[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(1):307-319. |
| APA | Guo, Rui-Hua.,Zhang, Quan.,Ma, Yun-Bao.,Luo, Jie.,Geng, Chang-An.,...&Chen, Ji-Jun.(2011).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,46(1),307-319. |
| MLA | Guo, Rui-Hua,et al."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 46.1(2011):307-319. |
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