Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloroquinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives

被引：114

作者：

Cheng, Pi ^{[1
,2
]}

Zhang, Quan ^{[1
,2
]}

Ma, Yun-Bao ^{[1
]}

Jiang, Zhi-Yong ^{[1
]}

Zhang, Xue-Mei ^{[1
]}

Zhang, Feng-Xue ^{[3
]}

Chen, Ji-Jun ^{[1
]}

机构：

[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

[3] Guangzhou Univ Tradit Chinese Med, Inst Trop Med Sci, Guangzhou, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 13期

基金：

中国国家自然科学基金;

关键词：

4-aryl-6-chloro-quinolin-2-one; 5-aryl-7-chloro-1,4-benzodiazepine; anti-HBV activity;

D O I：

10.1016/j.bmcl.2008.05.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-aryl-6-chloro-quinolin-2-ones and 5-aryl-7-chloro-1,4-benzodiazepine were synthesized and assayed for their in vitro anti-hepatitis B virus activities and cytotoxicities for the first time. Some of the tested compounds were active against HBsAg and HBeAg secretion in Hep G2.2.15 cells. Compound 5c showed IC50 of 0.074 and 0.449 mM on HBsAg and HBeAg secretions, respectively, which were 10 times higher than that of its analog 4c and led to better selective index (SI) values (SI = 23.2 and 3.4, respectively). (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3787 / 3789

页数：3

共 33 条

[11] QUINAZOLINES AND 1,4-BENZODIAZEPINES .22. A REARRANGEMENT OF 5-PHENYL-1,3-DIHYDRO-2H-1,4-BENZODIAZEPIN-2-ONES [J].