化学学报 ›› 2008, Vol. 66 ›› Issue (9): 1074-1078. 上一篇    下一篇

研究论文

青蒿素的生物素标记衍生物的合成

仲春龙1,2,姚祝军*,1,2   

  1. (1中国科学院上海有机化学研究所 上海 200032)
    (2中国科学技术大学化学系 合肥 230026)
  • 投稿日期:2007-11-05 修回日期:2007-12-29 发布日期:2008-05-14
  • 通讯作者: 姚祝军

Synthesis of the Biotinylated Artemisinin Derivative

ZHONG Chun-Long12 YAO Zhu-Jun*12   

  1. (1 State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032)
    (2 Department of Chemistry, University of Science and Technology of China, Hefei 230026)
  • Received:2007-11-05 Revised:2007-12-29 Published:2008-05-14
  • Contact: YAO Zhu-Jun

青蒿素1及其衍生物具有特征的过氧桥结构, 并呈现优秀的抗疟生物活性. 为了研究详细的作用机制和确定生物学作用靶标, 本研究从易得的青蒿素衍生物出发, 通过酰胺键相连, 合成了生物素标记的青蒿素衍生物.

关键词: 青蒿素, 生物素标记物, 合成, 靶标蛋白

Artemisinin (Qinghaosu, 1) and many of its derivatives, which contain a unique 1,2,4-trioxane unit, exhibit highly potent activities against multidrug-resistant malaria. In order to further understand their biological mechanisms and to identify their target proteins, a biotinylated derivative of artemisinin was synthesized, using a peptide-bond as the linkage between artemisinin and D-biotin.

Key words: artemisinin, biotinylated derivative, synthesis, target protein