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B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug
A Boumendjel1, F Bois, C Beney
1Département de Pharmacochimie Moléculaire UMR-CNRS 5063, UFR de Pharmacie de Grenoble, La Tronche, France. ahcene.boumendjel@ujf-grenoble.fr
Bioorganic & Medicinal Chemistry Letters
|January 5, 2001
Abstract:
Starting from the interaction of galangin (3,5,7-trihydroxyflavone) with a cytosolic nucleotide-binding domain of P-glycoprotein, a series of flavonol derivatives was synthesized and tested for their binding affinity towards the same target. The 5,7-dihydroxy-4'-iodoflavonol and 5,7-dihydroxy-4'-n-octylflavonol derivatives displayed much higher binding affinities, with respective increases of 6- and 93-fold as compared to galangin.