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1H NMR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 methylthiazolydiphenyl-tetrazolium bromide(MTT) method. The results show that most of the synthesized compounds have strong antitumor activities. Among them, the antitumor activities of compounds 4 and 6 are more potent than that of gambogic acid.
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