喹啉类化合物的合成及抗肿瘤活性研究

Synthesis and Antitumor Activity Evaluation of Quinoline Compounds

以间氟苯胺与乙氧基亚甲基丙二酸二乙酯为原料,经过缩合、高温环合、水解、高温脱羧、氯化,合成7-氟-4-氯-喹啉,7-氟-4-氯-喹啉与不同苯胺反应生成4个喹啉类化合物(J_1~J_4),其结构经过~1H NMR和MS确认.采用MTT法对目标化合物进行体外肿瘤细胞增殖抑制活性评价,结果显示目标化合物具有抑制肿瘤细胞增殖活性.

Using m-fluoroanline and ethoxym ethylene oxalic acid ester as starting material,7-fluoro-4-chloro-quinoline was synthesized through cyclization,high temperature cyclization,hydrolysis,high temperature decarboxylation,chlorination. Four quinoline compounds（ J1- J4） were synthesized by 7-fluoro-4-chloro-quinoline and different anilines,and their structures were confirmed by -1H NMR and MS. The antiproliferative activity of the compounds against three kinds of cancer cells（ SGC7901,HT1080,A549） was evaluated by MTT,and the results showthat the target compounds exhibited inhibitory activity of the three kinds of cancer cells.