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5-半乳糖基修饰环磷酰胺衍生物的合成及其抗肿瘤活性研究

郑愉, 孟祥豹, 李树春, 黄河清, 李中军*, 李庆*   

  1. 北京大学医学部 天然药物及仿生药物国家重点实验室; 药学院 化学生物学系, 北京 100191
  • 收稿日期:2010-05-31 修回日期:2010-07-30 出版日期:2010-09-20 发布日期:2010-09-20
  • 通讯作者: 李中军*, 李庆*

Synthesis and anti-tumor activities of 5-carbohydrate modified cyclophosphamide derivates

Yu Zheng, Xiang-Bao Meng, Shu-Chun Li, He-Qing Huang, Zhong-Jun Li*, Qing Li*   

  1. State Key Laboratory of Natural and Biomimetic drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2010-05-31 Revised:2010-07-30 Online:2010-09-20 Published:2010-09-20
  • Contact: Zhong-Jun Li*, Qing Li*

摘要: 本篇文章以5-苄氧基环磷酰胺为先导化合物, 通过连接臂4-羟基苄醇将肝靶向基团半乳糖基与环磷酰胺缀合, 设计合成了一类5-半乳糖苷苄氧基环磷酰胺类前药1a1b。期待从这些化合物中能筛选出具有肝靶向性和较好抗癌活性的环磷酰胺衍生物。

关键词: 环磷酰胺衍生物, 半乳糖苷, 肝靶向性, 抗癌活性

Abstract:

Novel prodrugs of cyclophosphamide 1a and 1b, which comprised the galactosyl moiety, the key fraction of cyclophosphamide derivates, and the linker 4-hydroxy benzaldehyde, were synthesized. These compounds were anticipated to exhibit amplified anti-tumor activity and targeting ability.

Key words: Cyclophosphamide, Galactoside, Hepatocyte targeting, Anti-tumor

中图分类号: 

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20732001, 90713004).
*Corresponding author. Tel.: 86-10-82801714