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含5-氟尿嘧啶生物可降解聚磷酰胺的合成及其抗肿瘤活性研究

Studies on the Synthesis and Antitumor Activity of Biodegradable Polyphosphamides

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【作者】 罗毅卓仁禧范昌烈

【Author】 LUO Yi;ZHUO Ren-xi;FAN Chang-Lie(Department of Chemistry,Wuhan University,Wuhan,430072)

【机构】 武汉大学化学系

【摘要】 通过L-赖氨酸(N ̄1-5-氟尿嘧啶)烷基酯双盐酸盐与二氯磷酸乙酯、二氯膦甲酸乙酯、二氯膦乙酸乙酯共聚,合成了三类12种侧链含5-氟尿嘧啶的聚磷酰胺。聚合物的结构经UV、IR、1HNMR及元素分析鉴定。聚合物用微量细胞培养四氮唑实验方法(MTT法)进行了对人肝癌细胞系Bel-7402细胞的微量培养实验。

【Abstract】 Twelve biodegradable polyphosphamides containing both 5-FU and phosphonoformic acid(or phosphonoacetic acid) ethyl ester were synthesized by condensation of L-lysine 5-FU alkyl(n=3,4,5,6)ester dihydrocmorides with dichloropliosplioric acid ethyl ester,dichlorophosphonoformic acid ethyl ester or dichlorophosphonoacetic acid ethyl ester,respectively,in DMF and in the presence of triethylamine. The drug release tests were studied in different pH media. Antitumor activities of monomer and polymers were tested against human hepatoma Bel-7402 cells in vitro.

【基金】 国家自然科学基金
  • 【分类号】R979.1
  • 【被引频次】29
  • 【下载频次】266
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