Isolation, Structure, Absolute Stereochemistry, and HIV-1 Integrase Inhibitory Activity of Integrasone, a Novel Fungal Polyketide
- 18 March 2004
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Natural Products
- Vol. 67 (5) , 872-874
- https://doi.org/10.1021/np0340504
Abstract
HIV-1 integrase is a critical enzyme for replication of HIV, and its inhibition is one of the most promising new drug targets for anti-retroviral therapy with potentially significant advantages over existing therapies. In this Note, the isolation, structure elucidation, and absolute stereochemistry of integrasone, a novel polyketide, derived from an unidentified sterile mycelium have been described. This bicyclic dihydroxy epoxide lactone inhibited the strand transfer reaction of HIV-1 integrase with an IC50 of 41 μM.Keywords
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