| 2-(4-三氟甲基苯基)-4-乙基-呋喃-3-酰胺衍生物的设计、合成及其抗肿瘤活性研究 |
| 投稿时间：2013-04-26 修订日期：2013-10-11 点此下载全文 |
| 引用本文：张涛,王甜甜,张一凯,牛春娟,李令振,李科.2-(4-三氟甲基苯基)-4-乙基-呋喃-3-酰胺衍生物的设计、合成及其抗肿瘤活性研究[J].药学实践杂志,2014,32(2):98~101,120 |
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| 基金项目:国家自然科学基金(81173559). |
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| 中文摘要:目的 设计、合成新型抗肿瘤的2-(4-三氟甲基苯基)-4-乙基-呋喃-3-酰胺衍生物。方法 以对三氟甲基苯甲醛和丙二酸二乙酯为起始原料,经缩合、环合、酰氯化及胺解等4步反应,合成系列目标化合物。结果 设计合成了15个目标化合物,并对其进行了4种肿瘤细胞A549、QGY、HeLa和SW480的活性测试。结论 显示出较好的抗肿瘤活性,化合物5b显示出最优的高效、广谱抗肿瘤活性,值得深入研究。 |
| 中文关键词:呋喃衍生物 化学合成 抗肿瘤 构效关系 |
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| Design, synthesis and anti-tumor activities of 2-(4-trifluoromethylphenyl)-4-ethyl-furan-3-amide derivatives |
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| Abstract:Objective To study the designing,synthesis and anti-tumor activities of the novel 2-(4-trifluoromethylphenyl)-4-ethyl-furan-3-amide derivatives. Methods 4-(trifluoromethyl)benzaldehyde and diethyl malonate were used as the starting materials to synthesize a series of target compounds through a multi-step reaction.Results 15 compounds were synthesized and their anti-tumor activities were tested against A549, QGY, HeLa and SW480 cell lines. Conclusion Target compounds showed good anti-tumor activities, compound 5b showed best broad spectrum activities, which was worth to continued study. |
| keywords:furan derivatives chemical synthesis anti-tumor structure-activity relationship |
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