摘要/Abstract

为了寻找结构新颖、活性较好的抗肿瘤化合物，设计合成了19个未见文献报道的3，4，5-三甲氧基苯基香豆素类化合物，并用核磁共振（NMR）和高分辨质谱（HRMS）等方法对化合物结构进行表征.用四甲基偶氮唑盐（MTT）法评价了该类化合物对人前列腺癌细胞（PC-3）、人食管癌细胞（EC-109）和人胃癌细胞（MGC-803）三种肿瘤细胞的抑制活性.结果显示，N-苄基-2-（（4-甲基-2H-色烯-2-酮-7-基）氧基）-N-（3，4，5-三甲氧基苯基）乙酰胺（4a）和N-（（5-氯苯并[b]噻吩-3-基）甲基）-2-（（4-甲基-2H-色烯-2-酮-7-基）氧基）-N-（3，4，5-三甲氧基苯基）乙酰胺（4n）对三种肿瘤细胞的抑制活性优于阳性对照药5-氟尿嘧啶，其中化合物4n对人前列腺癌细胞（PC-3）的抑制活性最好，其IC₅₀为4.18 μmol/L.
关键词: 香豆素, 抗肿瘤, 合成
Nineteen novel 3,4,5-trimethoxyphenyl coumarin derivatives have been synthesized and evaluated for antitumor activity against three human cancer cell lines (EC-109, PC-3 and MGC-803). These chemical structures were well characterized by NMR and HRMS spectroscopic methods. N-Benzyl-2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N-(3,4,5-trimethoxy-phenyl)acetamide) (4a) and N-((5-chlorobenzo[b]thiophen-3-yl)methyl)-2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N-(3,4,5-trimethoxyphenyl)acetamide) (4n) had better inhibitory activity against three kinds of tumor cells than 5-fluorouracil. Compound 4n showed the most potent antitumor activity against PC-3 cells with an IC₅₀ value of 4.18 μmol/L.
Key words: coumarin, anticancer, synthesis


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