| 于婷婷,李磊,崔华博,孟艳秋.化学通报,2017,80(11):1055-1060. |
| 熊果酸C-3,C-28位衍生物的合成及其抗肿瘤活性研究 |
| Synthesis of ursolic acid C-3, C-28 derivatives and their antitumor activity |
| 投稿时间：2017-04-17 修订日期：2017-09-05 |
| DOI： |
| 中文关键词: 熊果酸 合成 抗肿瘤活性 |
| 英文关键词:Ursolic acid Synthesis Anti-tumor activity |
| 基金项目:辽宁省自然科学基金（201605288）、沈阳市科学技术计划资助项目（F-16-230-6-00）、国家自然科学基金项目（21372156） |
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| 中文摘要: |
| 以天然产物熊果酸经过氧化、酰化、酯化等反应设计并合成了11个未见报道熊果酸衍生物, 其结构经过MS、1H-NMR及元素分析确定。以氟尿嘧啶和吉非替尼为阳性对照药, 经MTT法对A549和SGC-7901细胞进行初步体外抗肿瘤活性研究。结果表明,目标化合物对两种细胞株的抑制率均明显高于母体化合物，且化合物4b和5a的抑制效果高于阳性对照药，值得进一步研究。 |
| 英文摘要: |
| Eleven unreported derivatives of Ursolic acid were designed and synthesized by the oxidation, acylation and esterification of natural product Ursolic acid, meantime there structures were characterized by MS, 1H-NMR and elemental analysis. A549 and SGC-7901 cells were used to screen the anti-tumor activity in vitro through the MTT assay and compared with positive control drug 5-Fu and Gefitinib . The results indicated that these compounds have especially more potent inhibitory activity on A549 and SGC-7901 cells than Ursolic acid,especially the compound 4b and 5a showed more potent cytotoxicity than 5-Fu and Gefitinib, which are worthy to be studied further. |
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