多芳基取代咪唑的合成及其逆转多药耐药性研究

合成了一系列新的多芳基取代咪唑类化合物,其结构经元素分析、IR、¹HNMR和MS等确定,并采用MTT法测定了它们对由P-糖蛋白(P-gp)介导的肿瘤多药耐药性(MDR)的逆转效果.结果表明,化合物和具有很好的体外逆转MDR活性

Studies on Synthesis of Multiaryl-substituted Imidazoles and Reversal Activity on the Multidrug Resistance

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.