Synthesis and anti-HBV activity of S-substituted 7-mercapto-4-methylcoumarin analogs

被引：9

作者：

Chen, Ying ^{[1
]}

Zhou, Jin ^{[1
]}

Wang, Hai ^{[1
]}

Xia, Yi ^{[1
]}

Yang, Yu ^{[1
]}

Xia, Peng ^{[1
]}

机构：

[1] Fudan Univ, Dept Med Chem, Sch Pharm, Shanghai 200032, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2008年 / 19卷 / 08期

基金：

美国国家科学基金会;

关键词：

Synthesis; S-Substituted; 7-mercapto-4-methylcoumarin; Anti-HBV;

D O I：

10.1016/j.cclet.2008.05.043

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC50 values of sub-mu mol/L level. The IC50 of anti-HBsAg activities of 5c and 5j reached 0.01 mu mol/L respectively which were 16 fold more potent than that of 3TC. Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg. The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents. (C) 2008 Peng Xia. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

引用

页码：925 / 927

页数：3