摘要
本文通过十一种二羟基嘧啶衍生物单体与P,P-二氯膦甲酸乙酯进行缩聚反应,合成了十一种新的含5-氟脲嘧啶、尿嘧啶、胸腺嘧啶和膦甲酸乙酯的聚磷酸酯。用核磁、红外光谱及元素分析确定了聚合物的结构。进行了部分聚合物抗动物肿瘤活性试验,含5-氟脲嘧啶和膦甲酸乙酯的聚磷酯对小鼠艾氏腹水癌的抑制率可达56％。
New polyphosphates containing both pyrimidine base and phosphonoformic acidethyl ester were synthesized by the polycondensation of (ethoxycarbonyl) phosphonicdichloride(Ⅰ) with 1, 3-di(hydroxyalkyl)-5-fluorouracil(Ⅱ a,b,g), 1, 3-di(hydroxyalkyl)uracil(Ⅱ c,d), 1, 3-di(hydroxyalkyl)thymine (Ⅱ e,f), N,N'-di(2-thydroxyethyl)-5-fluorouracil-1, 3-diacetamide(Ⅲ a), N,N'-di(2-hydroxyethyl)uracil-1, 3-diacetamide(Ⅲ c) and N, N'-di(hydroxyalkyl)thymine-1, 3-diacetamide (Ⅲ e, f) respectively. Thechemical structure of these polyphosphates were confirmed by ~1H NMR and IR spectraas well as elementary analysis. All of the polymers of these polymers obtained are solublein water. The antitumor activity of some of these polymers were tested against Ehrlichascites carcinoma in vivo or in vitro.
出处
《功能高分子学报》
CAS
CSCD
1989年第1期67-72,共6页
Journal of Functional Polymers
关键词
抗肿瘤剂
聚磷酸酯
高分子药物
Antitumor agent
uracil
5-fluouracil
phosphonoformic acid
polyphosphate
thymine
polymeric drug
