Discovery, structure and HIV-1 integrase inhibitory activities of integracins, novel dimeric alkyl aromatics from Cytonaema sp.

Integrase is a critical viral enzyme for HIV-1 replication and is a novel target for therapeutic intervention against HIV infections. Integracins A–C are three novel dimeric alkyl aromatic inhibitors of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. These compounds inhibit both coupled and strand transfer activity of HIV-1 integrase with IC50 values of 3.2–6.1 and 17–88 μM, respectively. The discovery, structure and activity of these compounds are described.