Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase

被引：139

作者：

Singh, SB ^{[1
]}

Zink, DL ^{[1
]}

Goetz, MA ^{[1
]}

Dombrowski, AW ^{[1
]}

Polishook, JD ^{[1
]}

Hazuda, DJ ^{[1
]}

机构：

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

来源：

TETRAHEDRON LETTERS | 1998年 / 39卷 / 16期

关键词：

D O I：

10.1016/S0040-4039(98)00269-X

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Integration is an essential step in HN replication and is catalyzed by an enzyme called integrase. We have isolated equisetin (la), and a novel opposite stereochemical homolog, phomasetin (2a), from Fusarium heterosporum and a Phoma sp. respectively. They inhibit the invitro recombinant integrase enzyme with IC50 values of 7-20 mu M. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegration complexes isolated from HIV-I infected cells. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2243 / 2246

页数：4

共 12 条

[1]

BROWN PO, 1990, CURR TOP MICROBIOL, V157, P19

[2] ANTIBIOTIC PRODUCED BY FUSARIUM-EQUISETI NRRL-5537 [J].