两个α,β-不饱和酮药物的合成与活性研究

Synthesis and Activity of Two α,β- Unsaturated Ketone Drugs

本论文以2-甲氧基苯甲醛、4-甲氧基苯甲醛分别与4-三氟甲基苯甲醛、N-甲基-4-哌啶酮通过Claisen-Schmidt缩合反应得到两个不对称的α,β-不饱和酮化合物3-(4-三氟甲基苯亚甲基)-5-(2-甲氧基苯亚甲基)-N-甲基-4-哌啶酮(A)和3-(4-三氟甲基苯亚甲基)-5-(4-甲氧基苯亚甲基)-N-甲基-4-哌啶酮(B),并通过1H NMR、FTIR、元素分析等进行了充分的结构表征。MTT法评价其对人白血病细胞K562、人单核巨噬细胞THP-1等肿瘤细胞系的抗肿瘤活性及对人正常肝细胞LO2的细胞毒性。研究显示,A和B对K562、THP-1均具有较好的抑制活性。

Two asymmetric α,β- unsaturated ketone drugs（ 3E,5E）- 3-（ 4-（ trifluoromethyl） benzylidene）- 5-（ 2-methoxybenzylidene）- 1- methyl- 4- piperidone（ A） and（ 3E,5E）- 3-（ 4-（ trifluoromethyl） benzylidene）- 5-（ 4- methoxybenzylidene）- 1- methyl- 4- piperidone（ B） were prepared by Claisen- Schmidt condensation reaction of o-anisaldehyde or p- anisaldehyde,with 4-（ trifluoromethy） benzaldehyde and N- methyl- 4- piperidinone. They were characterized by1 H NMR,FTIR and elemental analysis. Their antitumor activities against human neoplastic cell lines K562,THP- 1 and their cytotoxicities for LO2 cell lines were evaluated by MTT method,which showed the better antitumor activities.