有机化学 ›› 2005, Vol. 25 ›› Issue (05): 549-553. 上一篇    下一篇

研究论文

含氨基酸席夫碱的5-氟尿嘧啶衍生物的合成及其抗肿瘤活性

石德清*,陈琦,李中华   

  1. (华中师范大学化学学院教育部农药与化学生物学重点实验室 武汉 430079)
  • 收稿日期:2004-07-12 修回日期:2004-11-15 出版日期:2004-04-30 发布日期:2004-04-30
  • 通讯作者: 石德清

Synthesis of Novel 5-Fluorouracil Derivatives Containing Amino Acid Schiff Base and Their Antitumor Activities

SHI De-Qing*,CHEN Qi,LI Zhong-Hua   

  1. (College of Chemistry, Central China Normal University and Key Laboratory of Pesticide and Chemical Biol-ogy,
    Ministry of Education of China, Wuhan 430079)
  • Received:2004-07-12 Revised:2004-11-15 Online:2004-04-30 Published:2004-04-30
  • Contact: SHI De-Qing

N 1-(2-四氢呋喃烷基)-5-氟尿嘧啶为原料, 与1,4-二溴丁烷反应, 得到N1-(2-四氢呋喃烷基)-N3-(4-溴丁基)-5-氟尿嘧啶(2), 最后与氨基酸席夫碱的钾盐缩合, 得到13个新的目标化合物3. 其结构经IR, 1H NMR, MS和元素分析确证. 初步的体外抗肿瘤试验结果表明, 目标化合物具有一定的抗肿瘤活性.

关键词: 5-氟尿嘧啶衍生物, 氨基酸席夫碱, 抗肿瘤活性

In order to search for novel high activity and low toxicity antitumor drugs, thirteen novel 5-fluorouracil derivatives containing amino acid Schiff base were synthesized via the condensation reactions of N 1-(2-furanidyl)-N 3-(4-bromobutyl)-5-fluorouracil and amino acid Schiff bases. The structures of the products were confirmed by IR, 1H NMR, MS spectra and elemental analyses. The result of preliminary bioassay shows that the new compounds possess antitumor activities to some extent.

Key words: 5-fluorouracil, antitumor activity, amino acid Schiff base