Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
Journal Article (Journal Article)
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 microM.
Full Text
Duke Authors
Cited Authors
- Herath, KB; Jayasuriya, H; Bills, GF; Polishook, JD; Dombrowski, AW; Guan, Z; Felock, PJ; Hazuda, DJ; Singh, SB
Published Date
- May 2004
Published In
Volume / Issue
- 67 / 5
Start / End Page
- 872 - 874
PubMed ID
- 15165153
International Standard Serial Number (ISSN)
- 0163-3864
Digital Object Identifier (DOI)
- 10.1021/np0340504
Language
- eng
Conference Location
- United States