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目的合成3,5-二亚苄基哌啶-4-酮类化合物,并对其体外抗肿瘤活性进行初步评价。方法以芳香醛、4-哌啶酮为原料,通过Claisen-Schmidt缩合制备目标化合物。采用MTT法测试目标化合物对人慢性粒细胞白血病急变细胞株K562增殖的抑制活性,考察部分化合物对多种肿瘤细胞株的抑制活性。结果与结论合成了7个未见报道的3,5-二亚苄基哌啶-4-酮类化合物,其结构经1H-NMR和MS谱确证;5个目标化合物的体外抗肿瘤活性明显强于姜黄素。
OBJECTIVE To synthesize 3,5-dibenzylidenepiperidin-4-ones and to evaluate the antitumor activity in vitro. Methods The target compounds were prepared by Claisen-Schmidt condensation using aromatic aldehyde and 4-piperidone as starting materials. The inhibitory activity of the target compounds on the proliferation of the human acute myeloid leukemia K562 cell line was tested by MTT assay and the inhibitory activity of some of the compounds on various tumor cell lines was investigated. RESULTS AND CONCLUSIONS Seven unreacted 3,5-dibenzylidenepiperidin-4-one compounds were synthesized and their structures were confirmed by 1H-NMR and MS. The antitumor activity of 5 target compounds in vitro was strong Curcumin.