齐墩果酸A环并咪唑类衍生物的合成及活性研究

Studies on the Synthesis and Activities of Azole Derivatives in Oleanolic Acid A Ring

以齐墩果酸为先导化合物,A环引入咪唑片段,28位酯化和生成酰胺结构,设计并合成3个新的衍生物,目标产物结构通过^(1)H-NMR确认.对所合成的目标化合物以人肺癌细胞(A549)和人肝癌细胞(HepG2)进行体外抗肿瘤活性测试,结果表明:目标化合物对两种肿瘤细胞的抑制活性均明显强于OA,化合物Ⅱ_(2)对HepG2细胞显示出较强活性(IC_(50)=22.32μmol/L).

Oleanolic acid was used as the lead compound to introduce imidazole fragment into a-ring.The structure of 28-site esterification and formation of amide was designed and synthesized,and three new derivatives were designed and synthesized.The structure of the target product was confirmed by ^(1)H-NMR.The antitumor activity of the synthesized target compound was tested in vitro on human lung cancer cells(A549)and human liver cancer cells(HepG2).The results showed that the inhibitory activity of the target compound on both tumor cells was significantly stronger than that of OA,and compound Ⅱ_(2) showed stronger activity on HepG2 cells(IC_(50)=22.32μmol/L).