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.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
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
