异维A酸二茂铁基衍生物的合成及其细胞毒活性的研究

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.

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

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.