目的 设计并合成了1，2，3-三氮唑类苦参碱衍生物，并对其进行体外抗肿瘤活性研究。方法 以苦参碱为起始原料，通过水解反应、N-烷基化反应、click反应等反应得到目标化合物。采用噻唑蓝（MTT）法考察所合成目标化合物对HeLa、MCF-7和HepG2 3种肿瘤细胞的体外抗增殖活性。结果 合成了9个1，2，3-三氮唑类苦参碱衍生物，其结构经¹H-NMR，¹³C-NMR及HR-MS确定，抗肿瘤活性测试结果表明该类化合物具有一定的抗肿瘤活性，其中化合物5h对MCF-7肿瘤细胞表现出良好的活性，且活性优于母体化合物苦参碱。结论 部分目标化合物具有较好的抗肿瘤活性，为该类抗肿瘤化合物的进一步优化提供思路。

Objective To devise and synthesize 1,2,3-triazole-substituted matrine derivatives and study the antitumor activities of the derivatives. Methods Taking matrine as the starting material, the target compounds were synthesized by hydrolysis reaction, N-alkylation reaction, and click reaction. Their antitumor activities of the synthesized target compounds were evaluated for HeLa, MCF-7, and HepG2 cells by MTT assay. Results Nine 1,2,3-triazole-substituted matrine derivatives were synthesized. Their structures were characterized by ¹H-NMR,¹³C-NMR, and HR-MS. MTT assay showed that some matrine derivatives exhibited antitumor activities. Compound 5h showed good antitumor activity against MCF-7 and was superior to the parent compound matrine. Conclusion Some derivatives have good antitumor activity and provide a basis for further optimization.

R914.2

国家自然科学基金资助项目（81502929）；中国医学科学院医学与健康科技创新工程经费资助项目（2016-I2M-3-015）