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

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	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-Hua 1,2; Zhang, Quan 1; Ma, Yun-Bao 1; Luo, Jie 1; Geng, Chang-An1,2 ; Wang, Li-Jun 1,2; Zhang, Xue-Mei1 ; Zhou, Jun1 ; Jiang, Zhi-Yong 1; Chen, Ji-Jun1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2011
卷号	46 期号:1 页码:307-319
关键词	Anti-hepatitis B virus activity Quinolin-2(1H)-one Structure-activity relationships
ISSN号	0223-5234
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
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.
学科主题	Pharmacology & Pharmacy
类目[WOS]	Chemistry, Medicinal
研究领域[WOS]	Pharmacology & Pharmacy
关键词[WOS]	IN-VITRO ; INHIBITORS ; HBV ; EXPRESSION ; DESIGN ; ALISOL
收录类别	SCI ; IC
资助信息	National Natural Science Foundation of China[81025023]; Chinese Academy of Sciences[GJHI200818, CAS-CF07/08.SC03]
语种	英语
WOS记录号	WOS:000286905400036
公开日期	2012-04-10
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/5385]
专题	昆明植物研究所_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.