Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase
Integration is an essential step in HIV replication and is catalyzed by an enzyme called integrase. We have isolated equisetin (1a), 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 μM. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegration complexes isolated from HIV-1 infected cells.
Singh, Sheo B.,Zink, Deborah L.,Goetz, Michael A.,Dombrowski, Anne W.,Polishook, Jon D.,Hazuda, Daria J.
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