Integrastatins: structure and HIV-1 integrase inhibitory activities of two novel racemic tetracyclic aromatic heterocycles produced by two fungal species

被引:66
|
作者
Singh, SB
Zink, DL
Quamina, DS
Pelaez, F
Teran, A
Felock, P
Hazuda, DJ
机构
[1] Merck Res Labs, Rahway, NJ 07065 USA
[2] Merck Sharp & Dohme Espana, CIBE, Madrid 28027, Spain
[3] Merck Res Labs, W Point, PA 19486 USA
关键词
D O I
10.1016/S0040-4039(02)00265-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Integrastatins are two novel aromatic natural products derived from fungal fermentations who possess a novel [6/6/6/6]-ring system and are racemic despite having two asymmetric centers. These compounds inhibited the strand transfer reaction of HIV-1 integrase with IC50 values of 1.1 -2.5 muM. (C) 2002 Published by Elsevier Science Ltd.
引用
收藏
页码:2351 / 2354
页数:4
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