(芳甲酰基)(羟基)喹啉酮类化合物的合成与生物活性研究  

Study on synthesis and biological activity of (arylformyl)(hydroxy) quinolinone derivatives

作　　者：黄二芳[1] 邢丽妍 张庆光[1] 张瑾[1] 黄健[1] 王金辉[1] 胡春[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国药物化学杂志》2015年第6期436-441,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(21342006)

摘　　要：目的设计合成具有抗肿瘤活性的(芳甲酰基)(羟基)喹啉酮类化合物。方法分别以6-羟基喹啉酮和7-羟基喹啉酮为原料,与对甲氧基苯甲酰氯成酯,利用无水三氯化铝经Fries重排同时脱甲基,再经Williamson反应得到目标化合物。采用MTT法,以乳腺癌细胞(MCF-7)为测试细胞株,对目标化合物进行体外抗肿瘤活性评价。结果与结论共合成了13个未见文献报道的(芳甲酰基)(羟基)喹啉酮类化合物,目标化合物的结构经质谱和核磁共振氢谱确证。活性评价结果显示,该系列化合物均有一定的抗肿瘤活性,其中,化合物4g,4j,4l活性较好。The design and synthesis of （arylformyl） （hydroxy） quinolinone derivatives as the anticancer agent were described herein. Thirteen target compounds were prepared via esterification, Fries rearrangement accom- panied by demethylation and Williamson reaction. The structures of all the target compounds were character- ized by 1H-NMR and ESI-MS data. Compounds 4g,4j and 41 showed significant biological activity against MCF-7 tumor cells with the inhibitory rates of 43.37% ,31.97% and 30. 89% ,respectively. The results showed that the （arylformyl） （hydroxyl） quinolinone derivatives were worthy to study the antitumor activities.

关 键 词：(芳甲酰基)(羟基)喹啉酮类化合物 分子对接 合成 选择性雌激素受体抑制剂 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]