藤黄酸氰基衍生物的合成及抗肿瘤活性  

Synthesis and Anti-tumor Evaluation of Nitrile-Containing Gambogic Acid Derivatives

作　　者：陈美君[1] 黎金海[1] 张志佳[1] 廖思燕[1] 黄雁[1] 谭茵[1] 

机构地区：[1]广州医科大学药学院,广州511436

出　　处：《应用化学》2016年第8期905-912,共8页Chinese Journal of Applied Chemistry

基　　金：广东省科技计划资助项目(2013B031800021)~~

摘　　要：以藤黄酸为原料，经过酯化反应或酰胺化反应，在C-30位的羧基上引入不同的烷氰基或芳香氰基，设计合成了7个藤黄酸氰基衍生物，其中6个为新化合物，其结构经MS和1HNMR确证。采用四氮唑蓝（MTT）法测试了合成化合物对肝癌细胞（HepG2）、结肠腺癌细胞（RKO）和卵巢腺癌细胞（OVCAR-3）的体外抗肿瘤活性，结果表明，所合成的化合物均具有一定的抗肿瘤活性，其中化合物4和6的抗肿瘤活性明显优于阳性对照物藤黄酸。Seven nitrile-containing gambogic acid derivatives were synthesized from gambogic acid （GA） through introducing different alkylnitriles or arylnitriles on the C-30 carboxyl of gambogic acid. Six of them are new compounds （1 --6）. Their structures were identified by 1H NMR and MS analysis. The evaluation of antitumor bioactivities in vitro on the hepatoma cells （HepG2）, colon adenocarcinoma cells （RKO） and ovarian adenocarcinoma cells （OVCAR-3） were done by the （MTT） method. The results show that most of the synthesized Among methyhhiazolydiphenyl-tetrazolium bromide compounds have strong antitumor activities. them, the antitumor activities of compounds 4 and 6 are more potent than that of gambogic acid.

关 键 词：藤黄酸 氰基 合成 抗肿瘤 衍生物 

分 类 号：O629.9[理学—有机化学]