| 熊果酸C-3,C-28位衍生物的合成及其抗肿瘤活性研究 |
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| 引用本文： | 于婷婷,李磊,崔华博,孟艳秋. 熊果酸C-3,C-28位衍生物的合成及其抗肿瘤活性研究[J]. 化学通报, 2017, 80(11): 1055-1060 |
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| 作者姓名： | 于婷婷 李磊 崔华博 孟艳秋 |
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| 作者单位： | 沈阳化工大学 制药工程教研室 辽宁 沈阳 110142,沈阳化工大学 制药工程教研室 辽宁 沈阳 110142,沈阳化工大学 制药工程教研室 辽宁 沈阳 110142,沈阳化工大学 制药工程教研室 辽宁 沈阳 110142 |
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| 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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| 摘 要： | 以天然产物熊果酸为原料,经过氧化、酰化、酯化等反应合成了11个未见报道的熊果酸衍生物,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。
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| 关 键 词： | 熊果酸 合成 抗肿瘤活性 |
| 收稿时间： | 2017-04-17 |
| 修稿时间： | 2017-09-05 |
Synthesis of ursolic acid C-3, C-28 derivatives and their antitumor activity |
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| YU Ting-ting,LI lei,CUI Hua-bo and MENG Yan-qiu. Synthesis of ursolic acid C-3, C-28 derivatives and their antitumor activity[J]. Chemistry, 2017, 80(11): 1055-1060 |
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| Authors: | YU Ting-ting LI lei CUI Hua-bo MENG Yan-qiu |
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| Affiliation: | Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology |
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| Abstract: | 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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| Keywords: | Ursolic acid Synthesis Anti-tumor activity |
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