新型藤黄酸衍生物的合成及其抗肿瘤活性

Synthesis and Antitumor Activities of Novel Gambogic Acid Derivatives

以藤黄酸（1）为原料,分别与HBr和有机胺反应,合成了9个新型的藤黄酸衍生物（2-6）,其结构经1HNMR,MS和HR-MS表征。采用MTT法测定了2-6对人结肠腺癌细胞（RKO）、人肝癌细胞（HepG-2）和人卵巢腺癌细胞（OVCAR-3）的体外抗肿瘤活性。结果表明,藤黄酸（N-丙基对甲苯磺酰胺）酯3,藤黄酸（N-丙基苯丙酰胺）酯4和N-色胺藤黄酰胺6b的抗肿瘤活性显著高于1;33-羟基转位藤黄酸2的抗肿瘤活性则大大降低。

Nine novel Gambogic acid derivatives（ 2 - 6） were synthesized by the reaction from Gambogic acid（ 1） with hydrobromic acid and organic amine,respectively. The structures were characterized by1 H NMR,MS and HR-MS. The in vitro antitumor activities of 2 - 6 against RKO,HepG-2and OVCAR-3 were investigated by the MTT method. The results showed that（ N-propyl-P-toluenesulfonamide） Gambogate（ 3）,（ N-propylphenylalaninamide） Gambogate（ 4） and N-tryptamine Gambogamide（ 6b） exhibited better antitumor activities than 1,while the activity of 30-hydroxygambogellic acid（ 2） remarkablely declined.