| 新型齐墩果酸衍生物的合成及其抗肿瘤活性 |
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| 引用本文： | 吕广颖,牟关敏,杨海君.新型齐墩果酸衍生物的合成及其抗肿瘤活性[J].合成化学,2012,20(4):416-420. |
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| 作者姓名： | 吕广颖 牟关敏 杨海君 |
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| 作者单位： | 西南科技大学材料科学与工程学院,四川绵阳,621010 |
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| 基金项目： | 国家自然科学基金资助项目，四川省非金属复合与功能材料重点实验室-省部共建国家重点实验室培育基地开放基金资助项目 |
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| 摘 要： | 以齐墩果酸(1)为原料,经3-羟基乙酰化,17-位羧基甲酯化,11-位碳羰基化及光照反应,首次实现了1的10-位角甲基的活化,合成了新型的齐墩果酸衍生物———3β-乙酰氧基-11α-羟基-11,25-环-齐墩果-12-烯-28-酸甲酯(4),其结构经1H NMR,13C NMR,IR和MS表征。采用SRB法测试了1～4及1的衍生物7～9对N-04,Bre-04和Lu-04细胞株的体外抑制活性,结果表明,4,8和9具有明显的抑制肿瘤细胞生长的能力。
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| 关 键 词： | 齐墩果酸 甲基活化 合成 抗肿瘤活性 |
Synthesis and Anticancer Activities of Novel Oleanolic Acid Derivative |
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| L Guang-ying
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MU Guan-min
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YANG Hai-jun.Synthesis and Anticancer Activities of Novel Oleanolic Acid Derivative[J].Chinese Journal of Synthetic Chemistry,2012,20(4):416-420. |
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| Authors: | L Guang-ying MU Guan-min YANG Hai-jun |
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| Institution: | L(U) Guang-ying
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MU Guan-min
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YANG Hai-jun |
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| Abstract: | A novel oleanolic acid(1) derivative,methyl 3β-acetoxy-11α-hydroxy-11,25-cyclo-olean-12-en-28-oate(4),was synthesized by acetylation of 3-hydroxyl,methyl-esterification of 17-carboxyl,carbonylation of C-11 and rradiation from 1.The structure was characterized by 1H NMR,13C NMR,IR and MS.The growth-inhibitory activities of 1~4 and derivatives(7~9) of 1 against N-04,Bre-04,and Lu-04 in vitro were determined by SRB assay.The results showed that 4,8 and 9 exhibited potent anti-tumor activities. |
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| Keywords: | oleanolic acid activation of methyl synthesis anti-tumor activity |
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