4-(甲基苯胺基)-3-氰基喹啉类衍生物的 合成及抗肿瘤活性

目的 设计合成4-(甲基苯胺基)-3-氰基喹啉类衍生物，并对其体外抗肿瘤活性进行初步评价。 方法 以氰乙酸乙酯为起始原料，经多步反应合成目标化合物。采用MTT法，以吉非替尼（gefitinib）为阳性对照药，以A549、HT-29和MDA-MB-231为测试细胞株对目标化合物的抗肿瘤活性进行了评价。 结果 合成了18个新化合物，经1H-NMR、MS和IR确认其结构。体外活性测试结果显示，多数化合物可在较低浓度抑制肿瘤细胞增殖，其中的Ⅶ2、Ⅶ3、Ⅶ6、Ⅶ12、Ⅶ13、Ⅶ15 和 Ⅶ16共7个化合物有显著的抗增殖活性，优于阳性对照药吉非替尼。 结论 体外活性实验表明：4-(甲基苯胺基)-3-氰基喹啉类衍生物作为新型的酪氨酸激酶抑制剂，其构效关系值得进一步研究。

Synthesis and anti-tumor activities of 4-(methylphenylamino) -quinoline-3-carbonitrile derivatives

Aim To design and synthesize a series of novel 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives,and to evaluate their antitumor activities.Methods The target compounds were synthesized via several steps with the starting material ethyl cyanoacetate,and their antitumor activities were examined against A549,HT-29 and MDA-MB-231 cell lines in vitro with gefitinib as positive control.Results Eigh-teen target compounds were synthesized and their structures were confirmed by 1H-NMR,IR and MS spectra.The...