Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp that inhibits HIV-1 integrase

被引：69

作者：

Singh, SB

Zink, DL

Heimbach, B

Genilloud, O

Teran, A

Silverman, KC

Lingham, RB

Felock, P

Hazuda, DJ

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck Res Labs, W Point, PA 19486 USA

[3] Labs Merck Sharp & Dohme Espana, Ctr Invest Bas, Madrid 28027, Spain

来源：

ORGANIC LETTERS | 2002年 / 4卷 / 07期

关键词：

D O I：

10.1021/ol025539b

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] HIV-1 integrase is a critical enzyme for viral replication, and its inhibition is an emerging target for potential antiviral chemotherapy. We have discovered a novel inhibitor, integramycin, from screening of fermentation extracts using an in vitro assay. Integramycin possesses a hexacyclic ring system and exhibited an IC50 value of 4 muM against HIV-1 integrase (strand transfer). The isolation, structure elucidation, stereochemistry, conformation, and biological activity has been described.

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页码：1123 / 1126

页数：4

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