异维A酸二茂铁基衍生物的合成及其细胞毒活性的研究  

Synthesis and Cytotoxic Activities of 13-cis-Retinoyl Ferrocene Derivatives

作　　者：梁盛宗[1] 忻鼎丞[1] 龙伯华[1] 向建南[1,2,3] 

机构地区：[1]湖南大学化学化工学院,长沙410082 [2]湖南大学生物医学工程中心,长沙410082 [3]湖南大学化学生物传感与计量学国家重点实验室,长沙410082

出　　处：《有机化学》2009年第7期1092-1095,共4页Chinese Journal of Organic Chemistry

基　　金：湖南省长沙市科技局(No.K0802152-31)资助项目

摘　　要：为降低异维A酸的毒副作用并提高其癌细胞毒活性以及增加其在生物体内的吸收,通过Mitsunobu反应,以高于80%的收率合成了8种新异维A酸二茂铁基衍生物,并进行了结构表征与确认.采用3-(4,5-二甲基噻唑-2)-2,5-二苯基四唑溴盐(MTT)法测试了它们对肺癌细胞(A549)等的癌细胞毒活性.结果显示,引入二茂铁基团后的异维A酸二茂铁基衍生物具有很好的癌细胞毒活性。In order to decrease toxicities of retinoids, enhance their physiological activities against cancer cells and increase absorbency in the organisms, eight novel 13-cis-retinoyl ferrocene derivatives were synthesized in yields higher than 80% through Mitsunobu reactions. Their structures were characterized and their cytotoxic activities were determined in vitro by an 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide （MTT） assay using human cancer lines including A549 cells lines etc. Results showed that the 13-cis-retinoyl ferrocene derivatives modified by ferrocene groups exhibited excellent cytotoxic activities against cancer cells.

关 键 词：异维A酸 二茂铁衍生物 MITSUNOBU反应 细胞毒活性 

分 类 号：TQ463[化学工程—制药化工] Q26[生物学—细胞生物学]