Nineteen curcumin analogs were designed and synthesized front aromatic aldehydes and 4-piperidone by claisen-schmidt condensation. Their structures were characterized by 1H-NMR and MS. Their antitumor activities in vitro were evaluated against K562 and SW1116 tumor cell lines by MTT assay. The results showed that compounds 1,2,3,4,5,9,14,18 had significantly better activity against K562 cells than EF-24(IC50 = l. 58 μmol·L-1). Compounds 7,10,11 were stronger than EF-24(IC50 = 11.7μmol ·L-1)on SW1116.%以芳香醛、4-哌啶酮为原料,Claisen-Schimidt缩合制备3,5-(E)-二亚苄基哌啶-4-酮类化合物.采用MTT法测试目标化合物对人类慢性粒细胞白血病急变细胞K562,人结肠癌细胞SW1 116增殖的抑制活性.化合物1-19的结构经核磁和质谱确证,化合物7、10、11对SW1 116的抑制活性比EF-24强,化合物1-5、9、14、18对K562的抑制活性均比EF-24强.
展开▼