Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity

…, C Gauthier, R Terreux, R Kachadourian…

Index: Valdameri, Glaucio; Gauthier, Charlotte; Terreux, Raphael; Kachadourian, Remy; Day, Brian J.; Winnischofer, Sheila M. B.; Rocha, Maria E. M.; Frachet, Veronique; Ronot, Xavier; Di Pietro, Attilio; Boumendjel, Ahcene Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3193 - 3200

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Citation Number: 43

Abstract

ABCG2 plays a major role in anticancer-drug efflux and related tumor multidrug resistance. Potent and selective ABCG2 inhibitors with low cytotoxicity were investigated among a series of 44 chalcones and analogues (1, 3-diarylpropenones), by evaluating their inhibitory effect on the transport of mitoxantrone, a known ABCG2 substrate. Six compounds producing complete inhibition with IC50 values below 0.5 μM and high selectivity for ...