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题名: Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents
作者: 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; null(陈纪军)1
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
关键词: Hepatitis B virus ; 4-Aryl-6-chloro-quinoline ; Derivatives ; Synthesis
英文摘要: 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.
出版日期: 2011-02-15
卷号: 19, 期号:4, 页码:1400-1408
语种: 英语
收录类别: SCI
学科分类: Biochemistry & Molecular Biology; Pharmacology & Pharmacy; Chemistry
ISSN号: 0968-0896
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/5521
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; Huang, XY; Luo, J; Wang, LJ; Geng, CA; Zhang, XM; Zhou, J; Jiang, ZY; Chen, JJ.Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents,BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(4):1400-1408
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