| 熊果酸衍生物的合成及抗肿瘤活性的研究 |
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| 作者姓名： | Meng YQ Liu D Bai ZW Cai LL Ai HR |
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| 作者单位： | 沈阳化工大学制药工程教研室; |
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| 基金项目： | 教育部留学回国人员基金(20080890); 省教育厅高等学校科学研究重点项目(L2010433) |
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| 摘 要： | 以天然产物熊果酸为先导化合物,经过氧化、酰化、酯化(酰化)、水解等反应设计合成了16个熊果酸衍生物,其中包括11个新五环三萜化合物,以HeLa、SKOV3和BGC-823细胞为靶细胞,MTT法进行初步的体外抗肿瘤活性研究。结果表明,化合物7a对HeLa细胞的抑制活性、化合物8a对SKOV3细胞的抑制活性均明显强于熊果酸,值得进一步研究。
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| 关 键 词： | 熊果酸 五环三萜化合物 抗肿瘤活性 |
Synthesis and anti-tumor activity of ursolic acid derivatives |
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| Meng YQ,Liu D,Bai ZW,Cai LL,Ai HR.Synthesis and anti-tumor activity of ursolic acid derivatives[J].Acta Pharmaceutica Sinica,2011,46(5):556-560. |
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| Authors: | Meng Yan-qiu Liu Dan Bai Zhong-wei Cai Ling-li Ai Hong-ru |
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| Institution: | MENG Yan-qiu,LIU Dan,BAI Zhong-wei,CAI Ling-li,AI Hong-ru(Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Shenyang 110142,China) |
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| Abstract: | Structure of natural product-ursolic acid was modified for increasing its antitumor activity.Ursolic acid was acylated,esterified,hydrolized or oxidized to obtain target pentacyclic triterpenoid compounds with different substitutes.Sixteen derivatives of ursolic acid were designed and synthesized including eleven new compounds.Anti-tumor activities of ursolic acid and these derivatives against HeLa,SKOV3 and BGC-823 cells in vitro were investigated by MTT assay.The results indicated that compounds 7a and 8a... |
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| Keywords: | ursolic acid pentacyclic triterpenoid anti-tumor activity |
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