高等学校化学学报 ›› 1990, Vol. 11 ›› Issue (5): 543-545.

• 研究简报 • 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:1989-01-11 出版日期:1990-05-24 发布日期:1990-05-24
  • 通讯作者: 卓仁禧

Synthesis and Antitumor Activity of Amino Acid 5-Fluorouracil-1,3-dipropyl Esters Hydrochloride

Zhao Rulin, Fan Changlie, Zhuo Renxi   

  1. Department of Chemistry, Wuhan University, Wuhan
  • Received:1989-01-11 Online:1990-05-24 Published:1990-05-24

摘要: 用氨基酸作抗癌药物载体以提高对癌细胞选择性的研究引起了人们的浓厚兴趣。在前文中[1、2],我们报道了5-氟尿嘧啶乙酰和丙酰氨基酸及其氨基酸的3-(N′-5-氟尿嘧啶基)-丙醇酯的合成及其抗肿瘤试验研究。本文将报道一系列氨基酸(5-氟尿嘧啶-1,3-双丙基)酯盐酸盐的合成及其体外抗肿瘤活性的研究。

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: Ten amino acid 5-fluorouracil-1,3-dipropyl esters hydrochloride were obtained by the reaction of N-protected salts of amino acid with 1,3-bis(w-bromopropyl)-5-fluorouracil in the DMF and then deprotecting with HCl-MeOH. The structures of these new compounds were characterized by 1H NMR, IR and UV spectra as well as elemental analysis. The antitumor activities of all of the compounds were tested against EAC in vitro, the preliminary results showed that some of the compounds exhibit certain anititumor activity.

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