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以芳醛与N-甲基-4-哌啶酮通过Claisen-Schmidt缩合得到两个不对称的N-甲基-4-哌啶酮化合物,并通过NMR、FT-IR、元素分析等进行结构表征。采用MTT法,评价了两种化合物对Hela(宫颈癌细胞)、HeP G2(肝癌细胞)、THP-1(人单核巨噬细胞)、SGC-7901(胃癌细胞)的抑制活性以及对LO_2(正常肝细胞)的细胞毒性。结果显示,3-(4-吡啶亚甲基)-5-(3-硝基苯亚甲基)-N-甲基-4-哌啶酮显示较好的抑制活性,特别是对THP-1的IC50=0.58μmol/L,而3-(2-噻吩亚甲基)-5-(3-硝基苯亚甲基)-N-甲基-4-哌啶酮的抑制活性稍差,但对正常细胞LO_2毒性较小。
Two asymmetric N-methyl-4-piperidone compounds were obtained by Claisen-Schmidt condensation of aryl aldehydes with N-methyl-4-piperidone and were characterized by NMR, FT-IR, elemental analysis and the like Characterization. The inhibitory activities of the two compounds against Hela (cervical cancer cell), HeP G2 (hepatoma cell), THP-1 (human monocyte-macrophage), SGC-7901 (gastric cancer cell) Normal liver cells) cytotoxicity. The results showed that 3- (4-pyridylmethylene) -5- (3-nitrobenzylidene) -N-methyl-4-piperidone showed better inhibitory activity, especially against THP-1 IC50 = 0.58 μmol / L, whereas the inhibitory activity of 3- (2-thienylidene) -5- (3-nitrobenzylidene) -N-methyl- LO 2 is less toxic to normal cells.