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Link to original content: https://pubmed.ncbi.nlm.nih.gov/1445308/
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Comparative Study
. 1992 Oct 30;188(2):631-7.
doi: 10.1016/0006-291x(92)91103-w.

Flavones are inhibitors of HIV-1 proteinase

R I Brinkworth  1 , M J Stoermer, D P Fairlie
Affiliations
Comparative Study

Flavones are inhibitors of HIV-1 proteinase

R I Brinkworth et al. Biochem Biophys Res Commun. .

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.

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