Prenylated xanthones as potential P-glycoprotein modulators |
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Authors: | Tchamo D N Dijoux-Franca M G Mariotte A M Tsamo E Daskiewicz J B Bayet C Barron D Conseil G Di Pietro A |
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Affiliation: | Laboratoire de Pharmacognosie, DPM (UMR 5063 CNRS-UJF), Université Grenoble I, Faculté de Pharmacie, La Tronche, France. |
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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. |
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