藤黄酸胺基醇酯的合成及其抗肿瘤活性  

Synthesis and biological evaluation of aminoalcohol gambogate as anti-tumor agents

作　　者：何黎琴[1,2] 吴亚先[2] 付俐[2] 王效山[2] 张奕华[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009 [2]安徽中医药大学安徽省现代中药重点实验室,合肥230031

出　　处：《中国药科大学学报》2013年第5期394-400,共7页Journal of China Pharmaceutical University

基　　金：安徽省教育厅自然科学重点科研项目(No.KJ2013A168)~~

摘　　要：以藤黄酸为原料,与相应的二溴烷烃反应得到藤黄酸溴代烷基酯,再将其与不同的胺反应得到20个藤黄酸胺基醇酯衍生物(3a^3t),其结构经IR、MS、1H NMR确证。采用MTT法测试目标化合物对肝癌细胞Bel-7402、SMMC-7721、Bel-7404、QGY-7701和HepG2的体外抗肿瘤活性。结果显示,大多数化合物表现出较强的抗肿瘤活性,其中化合物3c,3g,3h,3p和3t活性强于藤黄酸,3g和3h的抗肿瘤活性强于紫杉醇。Gambogic acid（GA）was treated with corresponding dibromoalkanes to form brominated compounds, which were coupled with various amines to generate the target compounds 3a-3t. Their structures were characterized by IR, MS and 1H NMR. The effects of the target compounds on the proliferation of human HCC Bel-7402, SMMC-7721, Bel-7404, QGY-7701 and HepG2 cells were evaluated in vitro by MTT assay using GA and taxol as positive controls. Most of the GA derivatives（3c, 3g, 3h, 3p, 3t）displayed more potent activity against liver cancer cells than GA, and the activities of 3g and 3h were even more potent than that of taxol.

关 键 词：藤黄酸 衍生物 抗肿瘤活性 合成 

分 类 号：R914[医药卫生—药物化学]