Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Cytosporic Acid, a Fungal Metabolite Produced by a Cytospora sp.

Journal of Natural Products
2003.0

Abstract

HIV-1 integrase is a critical enzyme for replication of HIV, and its inhibition has the potential to lead to an anti-retroviral therapy that has advantages over existing therapies. Cytosporic acid (1) is a polyketide-derived novel natural product that was isolated from a fermentation broth of the filamentous fungus Cytospora sp. collected from Puerto Rico. It inhibited strand transfer reaction of HIV-1 integrase with an IC(50) of 20 microM. The isolation, structure elucidation, relative stereochemistry, and activity of 1 are described.

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