2-苯氨基咪唑啉-5-酮衍生物的合成及抗肿瘤活性Synthesis and antitumor activity evaluation of imidazol-2-phenylamino-5-one derivatives
张雪,吴亚闯,韩潇琪,张国刚,赵燕芳
摘要(Abstract)：
目的设计并合成新型具有抗肿瘤活性的2-苯氨基咪唑啉-5-酮类化合物。方法以甘氨酸为起始原料,经环合、Knoevenagel缩合、N-烷基化、S-烷基化、取代5步反应合成2-苯氨基咪唑啉-5-酮类衍生物,并初步考察目标物对H460(人肺癌细胞)、HT29(人结肠癌细胞)以及A549(非小细胞肺癌细胞)的增殖抑制活性。结果与结论合成了11个未见文献报道的2-苯氨基咪唑啉-5-酮衍生物,化合物的结构经~1H-NMR、MS谱确证。体外活性测试结果显示,化合物1c、1e表现出较强的抑制细胞增殖活性,其对试验的3种肿瘤细胞的IC_(50)值分别为0.41、0.38(H460),0.41、0.66(HT29),1.44、0.75(A549)μmol·L~(-1),阳性对照药物顺铂(cisplatin)对3种肿瘤细胞的IC50值分别为0.22、0.62、0.35μmol·L~(-1)。初步探讨了目标化合物的构效关系,为进一步结构改造提供参考。
关键词(KeyWords)： 咪唑啉-5-酮;合成;抗肿瘤活性;构效关系
基金项目(Foundation): 国家自然科学基金项目(81202405)
作者(Author): 张雪,吴亚闯,韩潇琪,张国刚,赵燕芳
DOI: 10.14142/j.cnki.cn21-1313/r.2017.05.002
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