title: Flavones are inhibitors of HIV-1 proteinase.
abstract: Substituted gamma-chromones were found to weakly inhibit HIV-1 proteinase, an important enzyme in the replication and processing of the AIDS virus. Chromones bearing hydroxyl substituents and a phenolic group at the 2-position (flavones) were the most active compounds and structure-activity relationships for a limited series of flavone inhibitors are presented. Dixon plots are reported and a possible mechanism for flavone-induced inhibition is proposed. The results are also compared with those for some structurally related non-peptidic inhibitors of HIV-1 proteinase. Since some flavonoid compounds have already been shown to have antiviral activity against AIDS, the present observations of anti-HIV-1 proteinase activity may be particularly significant.
authors.affiliation: Centre for Drug Design and Development, University of Queensland, Brisbane, Australia.
authors.forename: R I
authors.initials: RI
authors.lastname: Brinkworth
authors.forename: M J
authors.initials: MJ
authors.lastname: Stoermer
authors.forename: D P
authors.initials: DP
authors.lastname: Fairlie
mesh_terms: D002867:Chromones / Q000494:pharmacology*; D005419:Flavonoids / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000201:enzymology*; D007700:Kinetics; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D002867:Chromones; D005419:Flavonoids; D017320:HIV Protease Inhibitors