目的 設(shè)計并合成了1，2，3-三氮唑類苦參堿衍生物，并對其進行體外抗腫瘤活性研究。方法 以苦參堿為起始原料，通過水解反應(yīng)、N-烷基化反應(yīng)、click反應(yīng)等反應(yīng)得到目標化合物。采用噻唑藍（MTT）法考察所合成目標化合物對HeLa、MCF-7和HepG2 3種腫瘤細胞的體外抗增殖活性。結(jié)果 合成了9個1，2，3-三氮唑類苦參堿衍生物，其結(jié)構(gòu)經(jīng)¹H-NMR，¹³C-NMR及HR-MS確定，抗腫瘤活性測試結(jié)果表明該類化合物具有一定的抗腫瘤活性，其中化合物5h對MCF-7腫瘤細胞表現(xiàn)出良好的活性，且活性優(yōu)于母體化合物苦參堿。結(jié)論 部分目標化合物具有較好的抗腫瘤活性，為該類抗腫瘤化合物的進一步優(yōu)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

國家自然科學(xué)基金資助項目（81502929）；中國醫(yī)學(xué)科學(xué)院醫(yī)學(xué)與健康科技創(chuàng)新工程經(jīng)費資助項目（2016-I2M-3-015）