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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
  • ISSN号：1003-1057
  • 期刊名称：《中国药学：英文版》
  • 时间：0
  • 分类：R916.41[医药卫生—药学]
  • 作者机构：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
  • 相关基金：This work was supported by the funds of National Natural Science Foundation of China （Grant No. 20732001,90713004）.
作者： 郑愉, 孟祥豹, 李树春, 黄河清, 李中军, 李庆
关键词： 环磷酰胺衍生物, 半乳糖苷, 肝靶向性, 抗癌活性, Cyclophosphamide, Galactoside, Hepatocyte targeting, Anti-tumor
中文摘要：

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凼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1a和1b。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。

英文摘要：

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.

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期刊信息
  • 《中国药学：英文版》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:北京大学药学院
  • 主编：王夔
  • 地址：北京市学院路38号
  • 邮编：100083
  • 邮箱：zggy@mail.bjmu.edu.cn
  • 电话：010-82801713
  • 国际标准刊号：ISSN：1003-1057
  • 国内统一刊号：ISSN：11-2863/R
  • 邮发代号:
  • 获奖情况:
  • 国内外数据库收录:
  • 被引量:708