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化学学报
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化学学报 ›› 2008, Vol. 66 ›› Issue (4): 459-464. 上一篇    下一篇

研究论文

β-榄香烯三羰基铼配合物的合成、放射化学合成及抗癌活性研究

任云峰1,2, 成康民1,2, 刘贵锋1,2, 孙艳红1, 沈玉梅*,1   

  1. (1中国科学院上海应用物理研究所放射性药物研究中心 上海 201800)
    (2中国科学院研究生院 北京 100049)
  • 投稿日期:2007-07-06 修回日期:2007-09-06 发布日期:2008-02-28
  • 通讯作者: 沈玉梅

Synthesis, Radiosynthesis and Anticancer Activity of β-Elemene Tricarbonyl Rhenium Complex

REN Yun-Feng1,2; CHENG Kang-Min1,2; LIU Gui-Feng1,2; SUN Yan-Hong1; SHEN Yu-Mei*,1   

  1. (1 Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800)
    (2 Graduate School of the Chinese Academy of Sciences, Beijing 100049)
  • Received:2007-07-06 Revised:2007-09-06 Published:2008-02-28

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以中草药有效成分β-榄香烯为起始原料, 经烯丙位的氯代反应及亲核取代反应在β-榄香烯母体上成功地引入含吡啶基的三齿螯合剂, 并与稳定的三羰基铼配位, 得到了一种新的铼(I)三齿配合物, 在此基础上利用铼的放射性同位素Re-188进行了放射性标记. 反应中间体及最终化合物分别用IR, 1H NMR, HRMS, HPLC或元素分析进行表征, 并对该化合物进行了初步的体外抗癌活性研究. β-榄香烯三羰基铼配合物的合成、放射化学合成及体外抗癌活性评价, 为探讨β-榄香烯体内靶点和作用机制提供了可能, 并为最终开发基于β-榄香烯的放射性药物奠定了基础.

关键词: β-榄香烯, 三羰基铼, Re-188, 放射化学合成, 抗癌活性

Starting from the Traditional Chinese Medicine β-elemene, a new kind of β-elemene tricarbonyl rhenium complex was prepared via halogenation and nucleophilic substitution reactions, followed by reaction with tricarbonyl rhenium. Under the similar reaction conditions, the radioactive β-elemene tricarbonyl rhenium complex was synthesized. All the compounds were characterized by IR, 1H NMR, HRMS, HPLC or elemental analysis. The anticancer activity of the target compound was observed in Hela and LLC lines in vitro. The β-elemene tricarbonyl rhenium complex provides the possibility to explore the anticancer mechanism of β-elemene and furthermore find a new kind of radiopharmaceuticals on basis of β-elemene.

Key words: β-elemene, tricarbonyl rhenium, Re-188, radiosynthesis, anticancer activity