Document Report Card

ID: ALA1147233

Journal: J Nat Prod

Title: Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.

Authors: Singh SB, Ondeyka JG, Schleif WA, Felock P, Hazuda DJ.

Abstract: Integracides, 4,4-dimethylergostane triterpenoids, are inhibitors of HIV-1 integrase, a critical enzyme in replication of HIV-1. The chemistry and structure-activity relationship of integracide B and related natural products are described. A charged group, e.g., a sulfate, carboxyl, or amino, is required for the HIV-1 integrase activity. These compounds showed HIV-1 integrase activity with IC(50) values in the range 4.8-15 muM and exhibited antiviral activity in a viral spread assay, but with only a small or no therapeutic window.

CiteXplore: 14575434

DOI: 10.1021/np030211s