咪唑类抗癌药物研究进展

Advance in research of imidazoles as anti-tumor agents

咪唑环广泛地出现在不同类型的药物中,显示出不同的药理活性,如抗癌、抗菌、抗真菌、抗病毒、抗寄生虫、拮抗组胺受体等。尤其作为抗癌药物,其研究日益活跃且发展迅速。文中综述了咪唑类化合物作为抗癌药物在放射增敏剂、法尼基转移酶抑制剂、细胞色素P450抑制剂、血管生成抑制剂、拓扑异构酶抑制剂、周期素依赖型蛋白激酶抑制剂及耐药逆转剂等方面的最新进展及其构效关系。

Imidazole ring appears extensively in various types of pharmaceutical agents. It displays diversity of pharmacological activities such as anti-tumor, antibacterial, antifungal, anti-virus, anti-parasitic, histamine receptor antagonizing actions. Especially, as anti-tumor agents, the researches of imidazoles are increasingly active, and the progress is very quick. This paper described the recent advance in the research of imidazoles as antitumor agents. Imidazoles act as radiosensitizers, farnesyltransferase inhibitors, cytochrome P450 inhibitors, angiogenesis inhibitors, topoisomerase （ToPo） inhibitors, cyclin dependent kinase inhibitors, resistance reversal agents and others. Their structures-activity relationships （SAR） were also mentioned.