Synthesis and biological evaluation of bifendate–chalcone hybrids as a new class of potential P-glycoprotein inhibitors

…, X Tang, H Peng, Y Ma, Y Lai, S Peng, Y Zhang

Index: Gu, Xiaoke; Ren, Zhiguang; Tang, Xiaobo; Peng, Hui; Ma, Yuanfang; Lai, Yisheng; Peng, Sixun; Zhang, Yihua Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 8 p. 2540 - 2548

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Citation Number: 18

Abstract

Overexpression of P-glycoprotein (P-gp) is one of the major problems to successful cancer chemotherapy. To find novel effective P-gp inhibitors, a series of bifendate–chalcone hybrids were synthesized and evaluated. Among them, the most active compound 8g had little intrinsic cytotoxicity (IC50> 200μM), and could increase accumulation of Rhodamine 123 in K562/A02 cells more potently than bifendate and verapamil (VRP) by inhibiting P-gp efflux ...