CAJ | 학술논문

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.
위강저이유A산적독부작용병제고기암세포독활성이급증가기재생물체내적흡수,통과Mitsunobu반응,이고우80%적수솔합성료8충신이유A산이무철기연생물,병진행료결구표정여학인.채용3-(4,5-이갑기새서-2)-2,5-이분기사서추염(MTT)법측시료타문대폐암세포(A549)등적암세포독활성.결과현시,인입이무철기단후적이유A산이무철기연생물구유흔호적암세포독활성.
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.