有机化学 ›› 2012, Vol. 32 ›› Issue (9): 1673-1677.DOI: 10.6023/cjoc201205031 上一篇    下一篇

研究论文

新型核苷和单糖 1,2,3-三唑寡聚缀合物的合成及抗肿瘤活性

金培元a, 卢金荣a, 赵长琦b, 巨勇a,c   

  1. a 清华大学化学系 生命有机磷化学及化学生物学教育部重点实验室 北京 100084;
    b 北京师范大学生命科学学院 北京 100875;
    c 兰州大学功能有机分子化学国家重点实验室 兰州 730000
  • 收稿日期:2012-05-25 修回日期:2012-07-02 发布日期:2012-06-21
  • 通讯作者: 巨勇 E-mail:juyong@tsinghua.edu.cn
  • 基金资助:

    国家自然科学基金(No.21172130)和国家重点基础研究发展规划(973 计划) (No.2012CB821600)资助项目

Synthesis and Antitumor Activities of Novel 1,2,3-Triazole-fused Oligoconjugates Based on Nucleoside and Saccharide

Jin Peiyuana, Lu Jinronga, Zhao Changqib, Ju Yonga,c   

  1. a Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084;
    b School of Life Science, Beijing Normal University, Beijing 100875;
    c State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 73000
  • Received:2012-05-25 Revised:2012-07-02 Published:2012-06-21
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21172130) and the National Program on Key Basic Research Project (973 Program) (No.2012CB821600)

利用“点击反应”合成了一系列核苷和单糖的1,2,3-三唑寡聚缀合物7~12,其结构经1H NMR,MS确认.对所合成化合物进行了抑制Hela宫颈癌细胞增殖的体外活性筛选,发现二(脱氧胸苷)乙二醚三唑缀合物11a具有较好的抑制活性,且明显优于其核苷母体3'-叠氮-3'-脱氧胸苷.

关键词: 寡聚, 缀合物, 点击化学, 抗肿瘤活性

Novel 1,2,3-triazole-fused oligoconjugates 7~12 based on nucleoside and saccharide were synthesized via click chemistry. The structures were confirmed by 1H NMR and MS, and their antitumor activities were assayed against cervix cancer HeLa cells in vitro. The preliminary bioassay test shows that only bis(triazole) nucleoside 11a considerably inhibited the growth of cervix cancer HeLa cells and was much better than azidothymidine.

Key words: oligomerization, conjugates, click chemistry, antitumor activity