Isolation,Structure,Absolute Stereochemistry,and HIV-1 Integrase Inhibitory Activity of Integrasone,a Novel Fungal Polyketide

摘要

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 IC_(50)of 41 muM.