咪唑类抗癌药物研究进展  

Advance in research of imidazoles as anti-tumor agents

作　　者：蔡佳利[1] 李硕[1] 周成合[1] 甘淋玲[2] 吴俊[1] 

机构地区：[1]西南大学化学化工学院 [2]西南大学药学院,重庆400715

出　　处：《中国新药杂志》2009年第7期598-608,共11页Chinese Journal of New Drugs

基　　金：重庆市自然科学基金(CSTC2007BB5369);西南大学人才引进基金(SWUB2006018);西南大学高新技术培育基金(XSGX0602)

摘　　要：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.

关 键 词：咪唑 硝基咪唑 苯并咪唑 抗癌 放射增敏剂 法尼基转移酶抑制剂 

分 类 号：R979.1[医药卫生—药品] R914.5[医药卫生—药学]