Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents
Guo, Rui-Hua1,2; Zhang, Quan1; Ma, Yun-Bao1; Huang, Xiao-Yan1; Luo, Jie1; Wang, Li-Jun1,2; Geng, Chang-An1,2; Zhang, Xue-Mei1; Zhou, Jun1; Jiang, Zhi-Yong1; Chen, Ji-Jun1
2011-02-15
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
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
资助信息National Natural Science Foundation of China[81025023]; Chinese Academy of Sciences[GJHI200818]; CAS-Croucher Fund[CAS-CF07/08.SC03]
学科领域Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmc.2011.01.006
收录类别SCI
语种英语
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS类目Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000287592100004
引用统计
被引频次:24[WOS]   [WOS记录]     [WOS相关记录]
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
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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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