目的寻找高效低毒的秋水仙碱抗肿瘤衍生物。方法秋水仙碱首先被转化为硫代秋水仙碱,然后硫代秋水仙碱通过水解得到7-(N-脱乙酰基硫代秋水仙碱),最后经胺的酰化得到目标化合物。用1H NMR,IR,MS和HR-MS确证了这些衍生物的结构,MTT法评价了目标衍生物的细胞毒性;用对小鼠肝癌H22和宫颈癌U14的抑制率评价了衍生物的体内抗肿瘤活性。结果合成了12个硫代秋水仙碱新衍生物。结论尽管一些硫代秋水仙碱衍生物的体外细胞毒性强于秋水仙碱,然而小鼠体内抑瘤活性却较低。 Aim To find colchicine antitumor derivatives with high efficiency and low toxicity. Methods Colchicine was first converted to thiocolchicine, and then thiocolchicine was hydrolyzed to give 7- (N-deacetylthiocolchicine), and finally acylation of the amine gave the target compound. The structures of these derivatives were confirmed by 1H NMR, IR, MS and HR-MS. The cytotoxicity of the target derivatives was evaluated by the MTT method. The in vivo anti-derivatives of the derivatives were evaluated using the inhibitory rates against mouse H22 and U14 Tumor activity. Results Twelve new thiocolchicine derivatives were synthesized. Conclusions Although some thiocolchicine derivatives are more cytotoxic in vitro than colchicine, the antitumor activity in mice is lower.