| 三尖杉碱和桥氧三尖杉碱衍生物的合成及抗肿瘤活性 |
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| 引用本文： | 叶仙蓉,吴克美.三尖杉碱和桥氧三尖杉碱衍生物的合成及抗肿瘤活性[J].药学学报,2003,38(12):919-923. |
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| 作者姓名： | 叶仙蓉 吴克美 |
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| 作者单位： | 中国医学科学院、中国协和医科大学,药物研究所,北京,100050 |
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| 摘 要： | 目的为了充分利用我国的三尖杉属植物资源,寻找高效低毒的抗肿瘤药物。方法对三尖杉碱和桥氧三尖杉碱进行了C3位的结构修饰,合成了C3具有紫杉醇侧链及其对映体的新酯碱化合物。结果共得到6个新化合物。药理筛选表明,化合物VIIIa,VIIIb,IXa和IXc对KB,HCT和Bel具有较高的细胞毒作用。结论新酯碱值得进一步探讨研究。
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| 关 键 词： | 三尖杉碱 桥氧三尖杉碱 紫杉醇侧链 |
| 收稿时间： | 2003-01-14 |
Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine |
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| YE Xian-rong,WU Ke-mei.Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine[J].Acta Pharmaceutica Sinica,2003,38(12):919-923. |
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| Authors: | YE Xian-rong WU Ke-mei |
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| Institution: | Institute of Materia Medica Chinese Academy of Medical Science, Peking Union Medical College, Beijing 100050, China. xianrongye@imm.ac.cn |
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| Abstract: | Aim To make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects. Methods The C_3 hydroxy groups of the cephlotaxine and drupacine were acylated by taxol side chain and its isomers to give a series of derivatives of cephlotaxine and drupacine. Results Six novel alkaloid esters were designed and synthesized. The pharmacological screening results showed that VIIIa, VIIIb, IXa and IXc exhibited significant activities on KB, HCT and Bel in vitro . Conclusion Novel alkaloid esters are worthy to be intensively studied. |
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| Keywords: | cephalotaxine drupacine taxol side chain |
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