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

Tetrahedron Letters
1998.0

Abstract

Integration is an essential step in HIV replication and is catalyzed by an enzyme caged integmse. We have isolated equisetin (la), and a novel opposite stere&tetnical homolog, phomasetin (2a), from Fusariun~ he~emsporum and a Phomu sp. respectively. They inhibit the invitro recombinant integrase enzyme with ICm values of 7-20 pM. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegmtion complexes isolated from HIV-l infected cells. 0 1998 Elsevier Science Ltd. All rights reserved.

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