3,28-di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents

被引:48
作者
Kashiwada, Y
Chiyo, J
Ikeshiro, Y
Nagao, T
Okabe, H
Cosentino, LM
Fowke, K
Lee, KH
机构
[1] Niigata Coll Pharm, Niigata 9502081, Japan
[2] Fukuoka Univ, Fac Pharmaceut Sci, Fukuoka 8140180, Japan
[3] BBI Biotech Res Labs, Gaithersburg, MD 20877 USA
[4] Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA
关键词
D O I
10.1016/S0960-894X(00)00635-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Four isomers of 3,28-di-O-(dimethylsuccinyl)-betulin were prepared and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. 3-O-(3', 3'-Dimethylsuccinyl)-28-O-(2", 2"-dimethylsuccinyl)-betulin (11) was the most potent anti-HIV compound with an EC50 value of 0.00087 muM and a TI value of 42,400. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:183 / 185
页数:3
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