Author/Authors :
D. Noungoué Tchamo، نويسنده , , M. -G. Dijoux-Franca، نويسنده , , A. -M. Mariotte، نويسنده , , E. Tsamo، نويسنده , , J. B. Daskiewicz، نويسنده , , C. Bayet، نويسنده , , Lutz Hecht and Laurence D. Barron، نويسنده , , G. Conseil، نويسنده , , Daniele A. Di Pietro and Stefano Rebay، نويسنده ,
Abstract :
Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure–activity relationships. Decreasing polarity enhanced the binding affinity for the P-glycoprotein C-terminal cytosolic domain since DMA derivatives were more active, but unsubstituted hydroxyl group close to the carbonyl was required for efficient activity.
