目的 设计并合成天然产物绿原酸的酰胺类衍生物，并对该系列化合物进行体外抗肿瘤活性研究。方法 以绿原酸为起始原料，经保护、缩合、脱保护3步反应制得目标产物。采用噻唑蓝（MTT）法，考察所合成的目标化合物对人宫颈癌HeLa细胞、人肝癌HepG2细胞和人盲肠腺癌HCT-8细胞3种肿瘤细胞的体外增殖活性的影响。结果 设计并合成了10个绿原酸取代的苯甲酰胺及苯乙酰胺类衍生物B1～B5、C1～C5，其结构均经¹H-NMR、¹³C-NMR及HR-ESI-MS确定。抗肿瘤活性测试结果表明，10个绿原酸衍生物对3株肿瘤细胞株表现出不同程度的抑制效果，其中衍生物B2对HeLa细胞表现出良好的活性，且活性优于阳性对照药顺铂，所有的衍生物均对HCT-8细胞表现出抑制作用，且均优于阳性对照药顺铂。结论 10个绿原酸衍生物均为新化合物，部分衍生物具有较好的抗肿瘤活性，值得进一步深入研究。

Objective To designe and synthesize the natural chlorogenic acid amide derivatives and evaluate the in vitro antitumor activities of these compounds. Methods Using chlorogenic acid as starting material, the target compounds were prepared through three steps of protection, condensation, and deprotection reactions. Their antitumor activities of the synthesized target compounds were evaluated for HeLa, HepG2 and HCT-8 cells by MTT assay. Results Ten chlorogenic acid-substituted benzamide and phenylacetamide derivatives B1-B5, C1-C5 were designed and synthesized. Their structures were determined by ¹H-NMR, ¹³C-NMR and HR-ESI-MS. MTT assay showed that ten chlorogenic acid derivatives exhibited antitumor activities. Derivative B2 showed good activity against HeLa tumor cells and was superior to the positive control drug cisplatin. All derivatives showed inhibitory effects against HCT-8 tumor cells, and were all better than cisplatin. Conclusion Ten chlorogenic acid derivatives were new compounds. Some derivatives have good antitumor activity and were deserved further research.

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北京市自然科学基金资助项目（7192129）；国家自然科学基金资助项目（81302656）；中国医学科学院医学与健康科技创新工程项目（2016-I2M-1-012）