三氮唑衍生物抗肿瘤作用及其机制的研究进展  

Research Progress of the Mechanism on Antitumor Activity of the Triazole Derivatives

作　　者：刘彬[1] 胡国强[2] 康玉华[3] 

机构地区：[1]河南大学护理学院神经生物学研究所,开封475004 [2]河南大学药物研究所,开封475004 [3]河南大学淮河临床学院,开封475001

出　　处：《药物生物技术》2009年第5期472-476,494,共6页Pharmaceutical Biotechnology

基　　金：国家自然科学基金资助课题(编号:0771140);河南省医学科技攻关计划项目(编号:200703080);河南省教育厅自然科学研究计划项目(编号:2008A31000)

摘　　要：综述三氮唑衍生物对肿瘤细胞增殖、凋亡和分化影响作用机制的研究进展。三氮唑类包括1,2,4-和1,2,3-结构类型,从结构修饰特点上可分为单杂环和稠杂环类型。构-效关系表明,1,2,4三氮唑和1,2,3三氮唑与其他取代基相缀合或并合,均可合成具有一定抗肿瘤活性的衍生物。三氮唑衍生物通过对肿瘤细胞多个靶点的进攻产生细胞毒性作用,抑制细胞增殖、阻断细胞周期、导致细胞的凋亡,部分三氮唑衍生物具有显著的诱导肿瘤细胞终末分化的作用。对其结构中的某些基团进行修饰可能导致其生物学效应发生改变,抑制与肿瘤细胞增殖相关酶的活性,这些研究进展可为进一步研究和开发应用此类化合物提供依据。The research progresses of the triazole derivative on the effect of tumor cell proliferation, apoptosis and differentiation were reviewed. The triazole derivatives include 1,2. 3 - triazol and 1,2. 4 - triazol. The compounds are classified as the single hetercyclc ring and the fused heterocyclic ring according to the structural modification characteristics. Structure-activity relationship indicated that antitumor triazole derivatives could be synthesized through both 1,2.3 - triazol and 1, 2.4 - triazol conjugated or fused with other substitutes. Through attacking multiple target of tumor cell, the triazole derivatives generate systemic toxicity resulting in inhibiting cell proliferation, and inducing the cell cycle arrest and apoptosis. Some triazole derivatives have effect on inducing terminal differentiation of the tumor cells. If some groups of triazole derivative＇s structure are modified, its biology action will be changed. The study will play an important role in guiding further development and utilization of triazole derivatives.

关 键 词：三氮唑衍生物 肿瘤 细胞增殖 细胞凋亡 细胞分化 

分 类 号：R915[医药卫生—微生物与生化药学]