Synthesis and Anticancer Activity of Novel Coumarin Derivatives
Synthesis and Anticancer Activity of Novel Coumarin Derivatives
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新型香豆素衍生物的合成及其抗癌活性
DOI：
10.6023/cjoc201911028
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发表时间：
2020
影响因子：
1.9
通讯作者：
Zhang Saiyang
中科院分区：
文献类型：
--
作者：
Shi Lei;Li Ziqiu;Cui Xinxin;Zhu Ting;Pang Xiaojing;Li Longhui;Luo Defu;Liu Fangfang;Zhao Bingyu;Long Yue;Zhang Saiyang
合成了19种新的3,4,5-三甲氧基苯基香豆素衍生物，并对3种人癌细胞（EC-109、PC-3和MGC-803）进行了抗肿瘤活性评价。这些化学结构通过核磁共振和HRMS光谱方法得到了很好的表征。N-苄基-2-（（4-甲基-2-氧- 2h - chromen7 -基）氧）-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-2-氧- 2h - chromen7 -基）氧）-N-（3,4,5三甲氧基苯基）乙酰胺)（4n）对3种肿瘤细胞的抑制活性均优于5-氟尿嘧啶。化合物4n对PC-3细胞的抗肿瘤活性最强，IC50值为4.18 μmol/L。
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-trimethoxyphenyl)acetamide) (4a) and N-((5-chlorobenzo[b]thiophen-3-yl)methyl)-2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N-(3,4,5trimethoxyphenyl)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.