摘要
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、1 H NMR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
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.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2004年第5期870-873,共4页
Chemical Journal of Chinese Universities
基金
广东省自然科学基金重点项目(批准号 :0 2 1813 )
教育部博士学科点基金项目(批准号 :2 0 0 10 5 5 80 0 5 )资助
