抗肿瘤前药-姜黄素衍生物的设计合成及初步活性测试

目的:为了提高姜黄素的抗癌活性及选择性,考虑将之做成前药形式.方法:从几种氨基酸出发,经过马来酸酐活化后与姜黄素结合,得到四个化合物.利用MTT法对四个目标化合物进行了体外抗肿瘤活性评价.结果与结论:其结构经IR,1HNMR和13CNMR确证.目标化合物对胰腺癌细胞株SW-1990和膀胱癌细胞株T24的抑制试验结果表明,四个化合物对这两种细胞的抑制作用均优于阳性对照药5-Fu.

Design, Synthesis, and Primary Evaluation on Curcumin Derivative as Prodrugs of Antitumor

Objective: To raise the antitumor activity and high selectivity for curcumin, it was feasible to synthesis the prodrug of curcumin. Method: Four new compounds were prepared respectively by reacting on curcumin with N-maleoyl L-amino acids. Their structures were confirmed by IR, 1 HNMR, and 13 CNMR spectra. Result & Conclusion: The four target compounds were tested preliminarily in vitro for their antitumor activity. The result showed that these compounds were more effective than curcumin and 5-Fu against human cancer cells.