Dimethoxyaurones: Potent inhibitors of ABCG2 (breast cancer resistance protein)

HM Sim, CY Lee, PLR Ee, ML Go

Index: Sim, Hong-May; Lee, Chong-Yew; Ee, Pui Lai Rachel; Go, Mei-Lin European Journal of Pharmaceutical Sciences, 2008 , vol. 35, # 4 p. 293 - 306

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Citation Number: 62

Abstract

A series of 4, 6-dimethoxyaurones were synthesized by reacting 4, 6-dimethoxybenzofuran- 3 (2H)-one with various benzaldehydes in a base-catalyzed aldol reaction. AZ configuration was assigned to the aurones based on spectroscopic and crystallographic data. The aurones were tested for their ability to modulate ABCG2 (breast cancer resistance protein)- mediated multidrug resistance in vitro. Several members (0.5 μM) increased the ...