EQUISETIN AND A NOVEL OPPOSITE STEREOCHEMICAL HOMOLOG PHOMASETIN, 2 FUNGAL METABOLITES AS INHIBITORS OF HIV-1 INTEGRASE

Authors
SINGH SB ZINK DL GOETZ MA DOMBROWSKI AW POLISHOOK JD HAZUDA DJ
Citation
Sb. Singh et al., EQUISETIN AND A NOVEL OPPOSITE STEREOCHEMICAL HOMOLOG PHOMASETIN, 2 FUNGAL METABOLITES AS INHIBITORS OF HIV-1 INTEGRASE, Tetrahedron letters, 39(16), 1998, pp. 2243-2246
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron letters → ACNP
ISSN journal
00404039
Volume
39
Issue
16
Year of publication
1998
Pages
2243 - 2246
Database
ISI
SICI code
0040-4039(1998)39:16<2243:EAANOS>2.0.ZU;2-A
Abstract
Integration is an essential step in HN replication and is catalyzed by an enzyme called integrase. We have isolated equisetin (la), and a no vel opposite stereochemical homolog, phomasetin (2a), from Fusarium he terosporum and a Phoma sp. respectively. They inhibit the invitro reco mbinant integrase enzyme with IC50 values of 7-20 mu M. Unlike known i nhibitors, these compounds also inhibit the integration reactions cata lyzed by preintegration complexes isolated from HIV-I infected cells. (C) 1998 Elsevier Science Ltd. All rights reserved.