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5-氟尿嘧啶乙酸对-硝基苯酯和5-氟尿嘧啶丙酸对-硝基苯酯分别与三种二肽反应,制备了五个5-氟尿嘧啶二肽(4 a-e)。以5-氟尿嘧啶的氨基酸对-硝基苯酯(2 a-c)分别和三种二肽反应,制得四个5-氟尿嘧啶三肽(5 a-d)。产物经元素分析、NMR、IR和UV鉴定。初步动物试验表明:5-氟尿嘧啶丙酰甘-苯丙二肽,5-氟尿嘧啶乙酰甘-甘-苯丙三肽和5-氟尿嘧啶乙酰缬-亮-甘三肽对小白鼠移植性艾氏腹水癌有一定的抑制作用。
Five 5-fluorouracil dipeptides (4 a-e) were prepared by reaction of p-nitrophenyl 5-fluorouracil acetate and p-nitrophenyl 5-fluorouracil propionate with three dipeptides respectively. Four 5-fluorouracil tripeptides (5 a-d) were prepared by reacting the 5-fluorouracil amino-p-nitrophenyl ester (2 a-c) with three dipeptides respectively. The product was characterized by elemental analysis, NMR, IR and UV. Preliminary animal experiments show that: 5 - fluorouracil propionyl Gan - phenylpropane dipeptide, 5 - fluorouracil acetylglycerol - Gan - phenyl tripeptide and 5 - fluorouracil acetyl valyl - light Gantri peptide transplanted Ehrlich ascites carcinoma in mice Have a certain inhibitory effect.