Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents

doi:10.1016/j.bmc.2011.01.006

	Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents
	Guo, Rui-Hua 1,2; Zhang, Quan 1; Ma, Yun-Bao 1; Huang, Xiao-Yan 1; Luo, Jie 1; Wang, Li-Jun 1,2; Geng, Chang-An1,2 ; Zhang, Xue-Mei1 ; Zhou, Jun1 ; Jiang, Zhi-Yong 1; Chen, Ji-Jun1
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
	2011-02-15
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY
ISSN	0968-0896
卷号	19 期号:4 页码:1400-1408
摘要	A series of 4-aryl-6-chloro-quinoline derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely the abilities to inhibit the secretion of HBV surface antigen (HBsAg), HBV e antigen (HBeAg), and replication of HBV DNA in HepG 2.2.15 cells. Most of the compounds exhibited moderate inhibitory activity against the secretion of HBsAg and HBeAg. Nine compounds (3, 5, 6, 7, 10, 14, 17, 20, 24) showed significant inhibition against HBV DNA replication with IC(50) values in the range of 4.4-9.8 mu M, which were comparative to that of positive control tenofovir. Of them, compounds 10, 17, and 20 had low cytotoxicities, resulting in high SI values, >551.2, >143.7, and >284.5, respectively. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.
关键词	Hepatitis b Virus 4-aryl-6-chloro-quinoline Derivatives Synthesis
学科领域	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
DOI	10.1016/j.bmc.2011.01.006
收录类别	SCI
语种	英语
WOS记录号	WOS:000287592100004
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/5521
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. Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(4):1400-1408.
APA	Guo, Rui-Hua.,Zhang, Quan.,Ma, Yun-Bao.,Huang, Xiao-Yan.,Luo, Jie.,...&Chen, Ji-Jun.(2011).Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents.BIOORGANIC & MEDICINAL CHEMISTRY,19(4),1400-1408.
MLA	Guo, Rui-Hua,et al."Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents".BIOORGANIC & MEDICINAL CHEMISTRY 19.4(2011):1400-1408.

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