4-Hydroxy-6-methoxyaurones with high-affinity binding to cytosolic domain of P-glycoprotein.

…, MA Lawson, D Trompier, H Baubichon-Cortay…

Index: Boumendjel, Ahcene; Beney, Chantal; Deka, Nabajyoti; Mariotte, Anne-Marie; Lawson, Martin Ata; Trompier, Doriane; Baubichon-Cortay, Helene; Di Pietro, Attilio Chemical and Pharmaceutical Bulletin, 2002 , vol. 50, # 6 p. 854 - 856

Full Text: HTML

Citation Number: 46

Abstract

A series of 4-hydroxy-6-methoxyaurones and 4, 6-dimethoxyaurones has been synthesised and tested for their binding affinity toward the nucleotide-binding domain of P-glycoprotein, an ABC (ATP-Binding Cassette) transporter which mediates the resistance of cancer cells to chemotherapy. These compounds differ from each other by the nature of the substituent on the aurone B-ring. The binding affinity seems to be linked to the nature of the substituent, ...