Boumendjel A, Bois F, Beney C, Mariotte A M, Conseil G, Di Pietro A
Département de Pharmacochimie Moléculaire UMR-CNRS 5063, UFR de Pharmacie de Grenoble, La Tronche, France.
Bioorg Med Chem Lett. 2001 Jan 8;11(1):75-7. doi: 10.1016/s0960-894x(00)00595-3.
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.
