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2025年6月13日 18:08 星期五
首页 > 过刊浏览>2019年第50卷第4期 >2019,50(4):821-828. DOI:10.7501/j.issn.0253-2670.2019.04.006
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槐果碱肉桂酸酯衍生物的合成与抗肿瘤活性研究

Synthesis and antitumor evaluation of sophocarpine-cinnamic acid ester derivatives as potential antitumor agents

发布日期：2019-02-23
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    [关键词]
    [摘要]
    目的 合成槐果碱肉桂酸酯衍生物，并对衍生物进行体外抗肿瘤活性评价。方法 以槐果碱为起始原料，通过氧化、酯化、N-烷基化、还原、缩合、水解、成盐等反应得到目标化合物。采用噻唑蓝（MTT）法考察所合成的目标化合物对HeLa、HepG2和A-549 3种肿瘤细胞的体外抗增殖活性。结果 合成了11个槐果碱肉桂酸酯衍生物，其结构经1H-NMR、13C-NMR及HRMS确定，活性测试结果表明，部分衍生物表现出良好的抗肿瘤活性，其中，化合物5g对3种肿瘤细胞均表现出良好的抗肿瘤活性，且活性优于阳性对照药顺铂。结论 部分衍生物表现出良好的抗肿瘤活性，化合物5g具有进一步研究价值。
    [Key word]
    [Abstract]
    Objective To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion Some derivatives showed promising antitumor activities and compound 5g was worth further studying.
    [基金项目]
    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（2016-I2M-3-015）
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