Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols

被引：24

作者：

Jia, Wei ^{[1
]}

Liu, Yajing ^{[1
]}

Li, Wei ^{[1
]}

Liu, Yan ^{[1
]}

Zhang, Dajun ^{[1
]}

Zhang, Peng ^{[1
]}

Gong, Ping ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab New Drugs Design & Discovery Liaoning Pro, Sch Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 13期

关键词：

6H-[1]Benzothiopyrano[43-b]quinolines; Synthesis; Anti-HBV agents; REPLICATION; INFECTION;

D O I：

10.1016/j.bmc.2009.05.001

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel 6H-[1]benzothiopyrano[4,3-b]quinoline derivatives were prepared and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in human hepatoblastoma-derived liver Hep-G2 cells. Compounds 10g, 10h, 10j, 10l and 10o were found to be potent anti-HBV compounds with IC50 values less than 50 mu M. The most promising compound was 10l, with an IC50 value of 14.7 mu M and a SI value of 12.4. This is the first report of the anti-HBV effects of 6H-[1]benzothiopyrano[4,3-b] quinolin-9-ols. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved.

引用

页码：4569 / 4574

页数：6

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