硝酸酯类NO供体型齐墩果酸衍生物的合成及抗肿瘤活性

Synthesis and antitumor activity of novel oleanolic acid-nitrate conjugates

以齐墩果酸为先导物,将其3位OH通过各种类型的连接基团与硝酸酯类NO供体偶联,合成了10个目标化合物(2,4,8a～8c,10,12,15a～15c)。结构均经IR,MS及1HNMR确证,并采用MTT法测定了偶联物的细胞毒性。结果显示,化合物8c对人肺癌细胞A549、人结肠癌细胞HT-29及人肝癌细胞SMMC-7721均具有较强的抗肿瘤活性,值得进一步研究。

A series of novel oleanolic acid-nitrate conjugates were synthesized by coupling nitrate with 3-OH of OA via various linkers,and their structures were determined by IR,MS and 1H NMR.The cytotoxicity of the synthetic derivatives against human cancer cells SMMC-7721,BEL-7402,A549 and HT-29 was evaluated by MTT assay.Preliminary experimental results showed that compound 8c was the most potent one,whose cytotoxicity against A549,HT-29 and SMMC-7721 was stronger than that of the positive control adriamycin.Compound 8c is a promising compound worthy of further study.