Trimethoxybenzanilide-based P-glycoprotein modulators: an interesting case of lipophilicity tuning by intramolecular hydrogen bonding

…, A Carotti, F Leonetti, R Perrone, F Berardi…

Index: Pellicani, Raffaella Zoe; Stefanachi, Angela; Niso, Mauro; Carotti, Angelo; Leonetti, Francesco; Nicolotti, Orazio; Perrone, Roberto; Berardi, Francesco; Cellamare, Saverio; Colabufo, Nicola Antonio Journal of Medicinal Chemistry, 2012 , vol. 55, # 1 p. 424 - 436

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Citation Number: 5

Abstract

One of the principal reasons for the chemotherapy failure is the overexpression of drug efflux pumps, ABCB1 (also known as MDR1 or P-gp) and ABCC1 (also known as MRP1), whose inhibition remains a priority to circumvent drug resistance. We have recently shown a clear trend between lipophilicity and P-glycoprotein inhibitory activity for a class of galloyl-based modulators targeting P-glycoprotein and MRP1. Herein we report a new series of ...