Anti-AIDS agents. Part 61: Anti-HIV activity of new podophyllotoxin derivatives

被引：40

作者：

Zhu, XK

Guan, J

Xiao, ZY

Costentino, LM

Lee, KH ^{[1
]}

机构：

[1] Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA

[2] Biotech Res Labs Inc, Rockville, MD 20850 USA

[3] Chinese Acad Med Sci, Dept Synthet Med Chem, Beijing 100050, Peoples R China

[4] Peking Union Med Coll, Beijing, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 15期

关键词：

D O I：

10.1016/j.bmc.2004.04.048

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 podophyllotoxin derivatives containing structural modifications at C-4 (7-14), C-4' (16-17), and the methylenedioxy A-ring (23-28) was synthesized and tested for inhibition of HIV replication. Four of these compounds (25-28) were previously reported to show EC50 values of <0.001 mug/mL and therapeutic index (TI) values >120. Three of the newly tested compounds (8.. 12, and 20) showed good activity with EC50 values of 0.012, <0.001, and 0.389 mug/ml and TI values of 19.1, >16, and 19.4, respectively. A comparison of the anti-HIV activity of these derivatives suggested that an opened A-ring with 6,7-dimethoxy substitution and a 4'-demethylated E ring enhanced anti-HIV activity. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4267 / 4273

页数：7

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