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  

Design,synthesis and anti-tumor activities of 2-(4-trifluoromethylphenyl)-4-ethyl-furan-3-amide derivatives

作　　者：张涛[1] 王甜甜[1] 张一凯[1] 牛春娟[1] 李令振 李科[1] 

机构地区：[1]第二军医大学药学院药物化学教研室,上海200433

出　　处：《药学实践杂志》2014年第2期98-101,120,共5页Journal of Pharmaceutical Practice

基　　金：国家自然科学基金(81173559)

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、He[a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。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, EleLa and SW480 cell lines. Conclusion Target compounds showed good anti-tumor activ- ities, compound 5b showed best broad spectrum activities, which was worth to continued study.

关 键 词：呋喃衍生物 化学合成 抗肿瘤 构效关系 

分 类 号：R914.5[医药卫生—药物化学]