Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2

…, A McLeer-Florin, V Bourgarel-Rey…

Index: Combes, Sebastien; Barbier, Pascale; Douillard, Soazig; McLeer-Florin, Anne; Bourgarel-Rey, Veronique; Pierson, Jean-Thomas; Fedorov, Alexey Yu.; Finet, Jean-Pierre; Boutonnat, Jean; Peyrot, Vincent Journal of Medicinal Chemistry, 2011 , vol. 54, # 9 p. 3153 - 3162

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Citation Number: 45

Abstract

A series of A-ring variously methoxylated 4-(3-hydroxy-4-methoxyphenyl) coumarins related to combretastatin A-4 was prepared by cross-coupling reactions. Cytotoxicity studies indicated a potent activity against HBL100 cell line. Substitution patterns on A-ring had only a slight effect on antiproliferative activity. For most cytotoxic compounds, the activity as potential modulators of P-gp and BCRP efflux pumps was evaluated. The results show ...