Design, synthesis and anti-tumor activities of 2-(4-trifluoromethylphenyl)-4-ethyl-furan-3-amide derivatives
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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。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.
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Key words:
- furan derivatives /
- chemical synthesis /
- anti-tumor /
- structure-activity relationship
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