Abstract: Multidrug resistance(MDR) is one of the major obstacles to successful chemotherapy treatment of tumour. One of the main causes of MDR is linked to the overexpression of P-glycoprotein( P-gp). This study aimed to synthesize and characterize a novel class of triaryl-substituted imidazoles, a kind of potent inhibitors of P-gp mediated MDR. Their structures were characterized by elemental analysis, IR, ¹H NMR and MS spectra. Their reversal activities on the P-gp mediated MDR were tested by MTT method. The results reveal that compounds Ⅱ and Ⅲ have remarkable reversal activity in vitro, without apparently enhancing the toxicity of the co-administered drugs. Hence, they hold great promise as a kind of MDR modulators for the treatment of P-gp mediated MDR cancers.

Key words: Multiaryl-substituted imidazoles, P-Glycoprotein(P-gp), Multidrug resistance(MDR), Reversal activity