Integracides:: Tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp.

被引：25

作者：

Singh, SB

Zink, DL

Dombrowski, AW

Polishook, JD

Ondeyka, JG

Hirshfield, J

Felock, P

Hazuda, DJ

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 07期

关键词：

D O I：

10.1016/S0968-0896(02)00529-1

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：

HIV-1 integrase is a critical enzyme in the replication of HIV-1. It is absent in the host cells and therefore is a good target for treatment of HIV-1 infections. Integracides are members of the tetracyclic triterpenoids family that were isolated from the fermentation broth of a Fusarium sp. Integracide A, a sulfated ester, exhibited significant inhibitory activity against strand transfer reaction of HIV-1 integrase. The discovery, structure elucidation including single crystal X-ray structure and HIV-1 inhibitory activity of these compounds are described. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1577 / 1582

页数：6

共 22 条

[21] Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity [J].

Singh, SB ;

Felock, P ;

Hazuda, DJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (03) :235-238

[22] 4-aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells [J].

Wai, JS ;

Egbertson, MS ;

Payne, LS ;

Fisher, TE ;

Embrey, MW ;

Tran, LO ;

Melamed, JY ;

Langford, HM ;

Guare, JP ;

Zhuang, LG ;

Grey, VE ;

Vacca, JP ;

Holloway, MK ;

Naylor-Olsen, AM ;

Hazuda, DJ ;

Felock, PJ ;

Wolfe, AL ;

Stillmock, KA ;

Schleif, WA ;

Gabryelski, LJ ;

Young, SD .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (26) :4923-4926

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