Synthesis and anticancer activity containing benzyl piperidone study of curcumin-related compounds  

作　　者：Daiying Zhou Suqing Zhao Xi Zheng Zhiyun Du Kun Zhang 

机构地区：[1]Guangdong Food and Drug Vocational College, Guangzhou 510520, China [2]Guangdong University of Technology, Guangzhou 510006, China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2015年第8期524-529,共6页中国药学（英文版）

基　　金：China National Science Foundation Grants （Grant No. 21272043）, The PhD Start-up Fund of Natural Science Foundation of Guangdong Province （Grant No. 2014A030310329） and by Medical Scientific Research Foundation of Guangdong Province （Grant No. B2014072）.

摘　　要：Sixteen curcumin-related compounds containing benzyl piperidone were synthesized and evaluated for their anticancer activity by the MTT assay towards cultured prostate cancer （PC-3）, pancreatic cancer （BxPC-3）, colon cancer （HT-29）, and lung cancer （H1299） cells. Compounds A1 and B3 exhibited potent growth inhibitory effects against these cells in culture. The IC50 values of these compounds were lower than 1 μM in all four cell lines.采用氮烷基化、羟基保护、醛酮缩合三步反应合成了16个新型单羰基姜黄素类似物,结构经质谱、核磁共振氢谱和共振碳谱等手段进行确认。并采用MTT染色法体外检测所合成的16个单羰基姜黄素类似物对人肺癌细胞H1299、结肠癌细胞HT-29、人胰腺癌细胞Bx PC-3和人前列腺癌细胞PC-3的抗癌活性。半数抑制浓度IC50值结果显示:所合成的16个姜黄素类似物对四种细胞均有较强的抑制作用,其中化合物A1和B3在四种细胞中的半数抑制浓度IC50均在1μmol/L以下。

关 键 词：Curcumin-related compounds SYNTHESIS Anticancer activity 

分 类 号：R916[医药卫生—药学]