Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.

Published

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

Pubmed Central ID

  • 15165153

Electronic International Standard Serial Number (EISSN)

  • 1520-6025

International Standard Serial Number (ISSN)

  • 0163-3864

Digital Object Identifier (DOI)

  • 10.1021/np0340504

Language

  • eng