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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
引用本文:赵儒林,范昌烈,卓仁禧.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[J].高等学校化学学报,1989(6).
作者姓名:赵儒林  范昌烈  卓仁禧
作者单位:武汉大学化学系 (赵儒林,范昌烈),武汉大学化学系(卓仁禧)
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-(N~1-5-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-(N~1-5-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:5-氟尿嘧啶  氨基酸  抗肿瘤活性

Synthesis of Amino Acid 5-Fluorouracil Esters Derivatives and Study on Their Antitumor Activity
Zhao Rulin,Fan Changlie,Zhuo Renxi.Synthesis of Amino Acid 5-Fluorouracil Esters Derivatives and Study on Their Antitumor Activity[J].Chemical Research In Chinese Universities,1989(6).
Authors:Zhao Rulin  Fan Changlie  Zhuo Renxi
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, IR and UV spectra, 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.
Keywords:5-Fluorouracil  Amino acid  Antitumor activity  
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