异维A酸糖基衍生物的合成及其细胞毒活性研究

采用两种方法合成了2类新的异维A酸糖基衍生物(5a~5d, 6a, 10a~10c, 11a), 并进行了结构表征与确认. 采用MTT法测试了它们对肺癌细胞(A549)等的细胞毒活性. 结果显示, 含有糖苷结构的异维A酸衍生物明显比含有糖酯结构的异维A酸衍生物具有更好的细胞毒活性; 将糖环上的乙酰基脱去后, 相应的化合物活性有明显提高.

Studies on the Synthesis and Cytotoxic Activities of 13-cis-Retinoyl Sugar Derivatives

In order to decrease the toxicities of retinoids and enhance the pharmaceutical effects,especially the cytotoxic activities,retinoic acids were modified by glycosyl groups.Nine new retinoyl sugar derivatives of 13-cis-retinoic acid(5a-5d,6a,10a10c,11a) were synthesized in good yields.Their structures were characterized and their cytotoxic activities were determined in vitro with MTT assay by using human cancer lines including A549 cells lines etc.The results show that glucoside derivatives exhibited interesting cytotoxic activities and their cytotoxic activities are stronger than glycosyl esters.Deactylation of compounds 5a and 10a also improved their bioactivities,respectively.