有机化学 ›› 1989, Vol. 9 ›› Issue (3): 259-262. 上一篇    下一篇

研究论文

含5-氟尿嘧啶短肽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
  • 发布日期:1989-06-25

Synthesis and antitumor activity of dipeptyl 5-fluorouracil-propyl (butyl)ester derivatives

ZHAO RULIN;FAN CHANGLIE;ZHUO RENXI   

  • Published:1989-06-25

5-氟尿嘧啶丙酰苷-苯丙二肽, 5-氟尿嘧啶乙酰甘-甘-苯丙三肽和缬-受-甘三肽对小鼠艾氏腹水癌有一定的抑制作用. 为寻找选择性更好的5-氟脲嘧啶肽类衍生物, 合成了二肽的5-氟尿嘧啶丙酯和丁酯盐酸盐. 该化合物具有抗胂瘤试验的选择性. 苯丙-甘二肽的5-氟尿嘧啶丙酯盐酸盐和缬-亮二肽的5-氟尿嘧啶丙酯盐酸盐对小鼠艾氏腹水癌的抑制率分别为89.4%和86.88%.

关键词: 氟脲嘧啶, 抗癌药,

Twenty new dipeptide 5-fluorouracilpropyl and -butyl ester hydrochlorides were prepared from 5-fluorouracilpropyl or -butyl esters of amino acids with N-protected amino acid anhydrides. The antitumor activities of five of them were tested against Ehrlich ascites carcinoma in mice. Phe-Gly-O-(CH2)3-5-fluorouracil and Val-Leu-O-(CH2)4-5-fluorouracil hydrochlorides showed an inhibition ratio of 89.4% and 86.8%, resp.

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