高等学校化学学报 ›› 1989, Vol. 10 ›› Issue (6): 605.

• 研究论文 • 上一篇    下一篇

氨基酸5-氟尿嘧啶酯类衍生物的合成及其抗肿瘤活性研究

赵儒林, 范昌烈, 卓仁禧   

  1. 武汉大学化学系
  • 收稿日期:1987-12-27 出版日期:1989-06-24 发布日期:1989-06-24
  • 通讯作者: 卓仁禧

Synthesis of Amino Acid 5-Fluorouracil Esters Derivatives and Study on Their Antitumor Activity

Zhao Rulin, Fan Changlie, Zhuo Renxi   

  1. Department of Chemistry, Wuhan University, Wuhan
  • Received:1987-12-27 Online:1989-06-24 Published:1989-06-24

摘要: 以N-保护的氨基酸钾盐与1-(ω-溴丙基)-5-氟尿嘧啶和1-(ω-溴丁基)-5-氟尿嘧啶反应,制备了18种氨基酸的ω-(N1-5-氟尿嘧啶基)-丙醇酯和丁醇酯的盐酸盐,并确定了它们的结构。动物试验的初步结果表明,酪氨酸、苯丙氨酸的3-(N1-5-氟尿嘧啶基)-丙醇酯盐酸盐对小鼠艾氏腹水癌的抑制率分别为88.1%和86.7%。

关键词: 抗癌药, 氨基酸, 5-氟尿嘧淀, 5-氟尿嘧啶, 氨基酸, 抗肿瘤活性

Abstract: Eighteen amino acid 5-fluoroiu-acil-propyl(butyl) ester hydrochlorides were synthesized by the reaction of N-protected salts of amino acids with 1-(w-bromopropyl)-5-fluorouracil and 1-(w-bromobutyl)-5-fluorouracil in DMF. The structures of these new compounds were characterized by 1H NMR, IRand UVspectra, as well as elemental analysis, Tyrosine and phenylalanine 5-fluorouracil-propyl ester hydrochlorides show an inhibition ratio of 88.1% and 86.7% respectively against Ehrlich Ascites Carcinoma in mice.

Key words: Antitumor agent, Aminoacid, 5-Fluorouracil, 5-Fluorouracil, Amino acid, Antitumor activity

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