【摘要】 在齐墩果酸A环和C-28位羧基设计引入五元氮杂环,合成了12个氮唑骈缀的齐墩果酸新衍生物,其化学结构经HRMS、1H NMR予以确认,采用MTT法评价了目标物对人胃癌细胞MKN-45、人宫颈癌细胞Hela、人口腔表皮样癌细胞KB、人乳腺癌细胞MCF-7和大鼠胶质瘤C6细胞的体外抗肿瘤活性.结果发现浓度为10μmol/L时,目标物体外的抗肿瘤活性较齐墩果酸得到一定提高,其中化合物Q2表现出较强的抗肿瘤活性.更多还原

【Abstract】 Twelve novel azole oleanolic acid derivatives are synthesized by introducing five-membered nitrogen heterocycles into ring A and C-28 position of oleanolic acid,and confirmed by HRMS,1 H NMR. Their anticancer activities in vitro on human gastric cancer cells MKN-45,human cervical cancer cell Hela,human epidermoid carcinoma cell KB,human breast cancer cells MCF-7 and rat glioma C6 cells are evaluated by MTT assay. The results show that when the concentration is 10 μmol/L,the anti-tumor activity of the target compounds is higher than that of oleanolic acid,and compound Q2 exhibits the strongest anti-tumor activity.更多还原