摘要
以天然产物齐墩果酸为起始原料,对其C-3位羟基、C-12位双键、C-28位羧基进行结构改造,合成了13个新的齐墩果酸衍生物。目标化合物结构经MS、1H NMR及元素分析确证。采用MTT法,选用高表达人癌细胞(SGC7901、MCF-7和A549)对目标化合物进行初步的体外抗肿瘤活性研究。结果表明,所测化合物对3种肿瘤细胞的抑制活性均明显强于齐墩果酸,其中化合物II2和II3对MCF-7和A549细胞表现出很强的抑制活性,明显高于已上市药物吉非替尼,值得进一步研究。
Thirteen novel oleanolic acid（OA） derivatives were designed and synthesized with modification at positions of C-3, C-12 and C-28 of OA. Their structures were confirmed by MS, 1H NMR and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines（SGC7901, MCF-7 and A549） were evaluated by MTT assay. The results indicated that the tested derivatives were found to have stronger cell growth inhibitory activity than OA. Among them, compounds II2 and II3 showed more potent cytotoxicity on MCF-7 and A549 tumor cells than gefitinib（positive control）. They are worthy to be studied further.
出处
《药学学报》
CAS
CSCD
北大核心
2015年第4期469-474,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(21372156)
辽宁省教育厅高等学校优秀人才支持计划资助项目(LR2013017)
沈阳市科技计划资助项目(F13-316-1-47)
