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.
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, 1H 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.
作者
雷蕾
徐阳荣
张建强
刘智
王洪波
孟庆国
LEI Lei;XU Yang-rong;ZHANG Jian-qing;LIU Zhi;WANG Hong-bo;MENG Qing-guo(Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China;State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China)
出处
《烟台大学学报（自然科学与工程版）》
CAS
2019年第2期129-135,共7页
Journal of Yantai University(Natural Science and Engineering Edition)
基金
国家自然科学基金资助项目(81728020)
山东省自然科学基金资助项目(ZR2018LH025)
