姜黄素类似物合成与体外抗肿瘤活性研究  

Synthesis and antitumor activity in vitro of curcumin analogs

作　　者：刘洋[1] 许建华[2,3] 黄秀旺[3] 刘锋[2] 吴梅花[2] 

机构地区：[1]福建医科大学药学院药物化学系,福建福州350004 [2]福建医科大学药学院药理学系,福建福州350004 [3]福建医科大学新药研究所,福建福州350004

出　　处：《化学研究与应用》2011年第7期923-927,共5页Chemical Research and Application

基　　金：福建省教育厅项目(JA10150)资助;福建省科技重点项目(2009Y0025)资助

摘　　要：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SW1116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SW1116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。Nineteen curcumin analogs were designed and synthesized from 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=1.58 μmol·L-1）.Compounds 7,10,11 were stronger than EF-24（IC50=11.7 μmol·L-1）on SW1116.

关 键 词：姜黄素 姜黄素类似物 EF-24 3 5-(E)-二亚苄基哌啶-4-酮 抗肿瘤活性 

分 类 号：O626.3[理学—有机化学]