title: Prenylated xanthones as potential P-glycoprotein modulators.
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.
authors.affiliation: Laboratoire de Pharmacognosie, DPM (UMR 5063 CNRS-UJF), Université Grenoble I, Faculté de Pharmacie, La Tronche, France.
authors.forename: D N
authors.initials: DN
authors.lastname: Tchamo
authors.forename: M G
authors.initials: MG
authors.lastname: Dijoux-Franca
authors.forename: A M
authors.initials: AM
authors.lastname: Mariotte
authors.forename: E
authors.initials: E
authors.lastname: Tsamo
authors.forename: J B
authors.initials: JB
authors.lastname: Daskiewicz
authors.forename: C
authors.initials: C
authors.lastname: Bayet
authors.forename: D
authors.initials: D
authors.lastname: Barron
authors.forename: G
authors.initials: G
authors.lastname: Conseil
authors.forename: A
authors.initials: A
authors.lastname: Di Pietro
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014970:Xanthines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D014970:Xanthines