刘剑敏    姜凤超

（华中科技大学同济医学院药物化学教研室   武汉 430030）

[摘 要] 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：本文从几种氨基酸出发，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4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，4个化合物对这两种细胞的抑制作用均优于对照品临床上常用的抗肿瘤药5－Fu。

关键词：前药 姜黄素衍生物 马来酸酐 合成 抗瘤活性

Design, Synthesis and Primary Evaluation of Curcumin Derivatives as  Prodrugs of Antitumor

LIU Jian min, JIANG Feng chao

(Department of Pharmacy, Tongji Medical College of Huangzhong Science & Technology University，Wuhan 430030,P.R.China)

[Abstract] Purpose: To get stronger anti-tumor activity and high selectivity, we considered that it should be feasible to synthesis the prodrug of curcumin. Method: Four new compounds were prepared respectively by reacting curcumin with N-maleoyl L-amino acids. Their structures were confirmed by IR, ¹HNMR and ¹³CNMR spectra. Results and conclusions: Four of the target compounds were tested preliminarily in vitro for their antitumor activity. The result showed that these compounds are more effective than curcumin and 5-Fu against human cancer cells.