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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (10): 1894-1898.DOI: 10.6023/cjoc201203001 上一篇    下一篇

研究论文

嘧啶衍生物对牛蒡子苷元片段修饰的研究

王欢欢a, 吴平a, 康宏b, 许亮a, 朱瑞新a,b, 康廷国a   

  1. a 辽宁中医药大学药学院 大连 116600;
    b 同济大学生命科学与技术学院 上海 200092
  • 收稿日期:2012-03-19 修回日期:2012-05-29 发布日期:2012-10-27
  • 通讯作者: 朱瑞新, 康廷国 E-mail:rxzhu@tongji.edu.cn
  • 基金资助:

    国家自然科学基金(No. 30976611)、中国高等教育博士研究基金计划(No. 20100072120050)和上海中药现代化(No. 09dZ1972800)资助项目.

Modify a Fragment of Arctigenin with Pyrimidine Derivatives

Wang Huanhuana, Wu Pinga, Kang Hongb, Xu Lianga, Zhu Ruixina,b, Kang Tingguoa   

  1. a School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600;
    b School of Life Sciences and Technology, Tongji University, Shanghai 200092
  • Received:2012-03-19 Revised:2012-05-29 Published:2012-10-27
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 30976611), the Research Fund for the Doctoral Program of Higher Education of China (No. 20100072120050) and the Traditional Chinese Medicine Modernization of Shanghai (No. 09dZ1972800).

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用一系列具有生物活性的嘧啶衍生物修饰牛蒡子苷元, 旨在寻找增强牛蒡苷元子抗肿瘤活性的同时又能降低嘧啶抗肿瘤副作用的先导化合物. 本研究通过把卤代后的嘧啶衍生物与牛蒡子苷元酚羟基相接, 合成得到11个新的化合物, 通过1H NMR与LC-MS表征确定其结构. 最终, 增加了牛蒡子苷元抗肿瘤化合物库中化合物的数量, 为接下来的体外活性筛选做准备.

关键词: 牛蒡子苷元, 结构修饰, 嘧啶衍生物, 异分子孪生药物

In order to enhance the anti-tumor activity of the arctigenin and reduce the side effects of pyrimidine, arctigenin was modified with pyrimidine derivatives having biological activities. In this research, some halogenated pyrimidines were linked to the phenolic hydroxyl group of the arctigenin to gain eleven new compounds, and the structures of them were identified by LC-MS and 1H NMR. So, the number of the anti-tumor compound libraries of compounds based on arctigenin was increased, and these compounds were prepared for the in-vitro activity screening in the near future. By our work, when enhance the alkalinity and increase the water content in DMF, the etherification reaction is promoted, to a certain extent.

Key words: arctigenin, structural modification, pyrimidine derivatives, nonidentical twin drug