Synthesis and anti-HIV activity of oleanolic acid derivatives

被引：120

作者：

Zhu, YM

Shen, JK

Wang, HK

Cosentino, 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, Gaithersburg, MD 20877 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(01)00647-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thirteen oleanolic acid derivatives were prepared and evaluated for anti-HIV activity in H9 lymphocytes. Saturating the C-12-C-13 double bond and converting the C-17-carboxyl group to an aminomethyl group led to compounds 13-15 and 19-20. respectively, which showed improved anti-HIV activity. Compound 15 was the most potent derivative with EC50=0.0039 mug/mL and TI = 3570. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：3115 / 3118

页数：4

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