【摘要】 对两种含氟芳酰胺季鏻盐的合成方法进行优化研究,并检测其体外抗肿瘤活性.为获得符合药学研究要求的目标化合物氯化-N-间三氟甲基苯基-3-丙酰胺基三苯基鏻和氯化-N-间三氟甲基苯基-4-丁酰胺基三苯基鏻,通过控制反应条件,改进分离方法,减少了副反应,提高了产率和产品纯度.采用CCK8法测试目标化合物对人表皮癌细胞(A431)、人脑星形胶质母细胞瘤细胞(U87-MG)、人肝永生化细胞(THLE-2)、人肝癌细胞(QGY-7701)、人肺退行性癌细胞(CALU-6)、人结肠癌细胞(SW-480)、人子宫内膜癌细胞(ISHIKAWA)、人胃癌细胞(NCI-N87)、人乳腺癌细胞(MDA-MB-231)和人肝癌细胞(Hep G2)的体外抗肿瘤活性.结果表明,目标化合物对THLE-2、A431和NCI-N87抑制活性较强,其中,丙盐表现出较强的抗肿瘤活性,值得进一步深入研究.更多还原

【Abstract】 The objective is to find the optimized method to synthesize two kinds of fluorinated aromatic amide quaternary phosphonium salts,and to detect their antitumor activity in vitro. In order to obtain target compounds meeting the pharmaceutical research requirements, chlorine-N-m-trifluoromethylphenyl-3-propylamide triphenylphosphonium and chlorine-N-m-trifluoromethylphenyl-4-butylamide triphenylphosphonium,side reactions are reduced,and the yield and product purity are improved by optimizing the reaction conditions and the separation process. CCK8 method is used to test the antitumor activity of the target compounds in vitro on human skin cancer cells (A431),the brain star glioblastoma cells (U87-MG),liver cell (THLE-2),immortalized human liver cancer cells (QGY-7701),degenerative lung cancer cells (CALU-6),human colon cancer cells (SW-480),human endometrial cancer cell (on),human gastric cancer cells (NCI-N87),human breast cancer cells (MDA-MB-231) and human liver cancer cells (Hep G2). The results indicated that the target compound had strong inhibitory activity against THLE-2,A431 and NCI-N87,among which propyl salt showed strong anti-tumor activity,which was worthy of further study.更多还原