氨基酸甲酯取代的尿苷及其衍生物的合成方法及应用  

Synthesis and application of amino acid methyl ester substituted uridine and its derivatives

作　　者：路博华 郭晓河[1] 梁炳玉 李玉江[1] 陶乐[1] 董黎红[1] 张胜前[2] LU Bohua;GUO Xiaohe;LIANG Bingyu;LI Yujiang;TAO Le;DONG Lihong;ZHANG Shengqian(High&New Technology Research Center of Henan Academy of Sciences,Zhengzhou 450002,Henan,China;North China University of Water Resources and Electric Power,Zhengzhou 450046,Henan,China)

机构地区：[1]河南省科学院高新技术研究中心,河南郑州450002 [2]华北水利水电大学,河南郑州450046

出　　处：《化学研究》2023年第6期482-489,共8页Chemical Research

基　　金：河南省科学院基本科研费项目(220602011,230602007);河南省科技攻关项目(232102310380)。

摘　　要：针对目前临床中所面临的耐药性问题,为开发具有抗肿瘤活性的新型结构化合物,以尿苷为原料,首次合成出具有新型结构的氨基酸甲酯取代的尿苷及其衍生物,反应路径合理,后处理简单;对合成的目标化合物进行了初步的抗肿瘤活性实验,结果显示设计合成的甘氨酸甲酯取代的尿苷对肿瘤有一定的抑制作用,为抗肿瘤药物研究奠定重要的基础。In order to develop novel structural compounds with anti-tumor activity,uridine and its derivatives with substituents of amino acid methyl ester were synthesized for the first time from uridine.The reaction path was reasonable and post-treatment was straightforward.The synthesized target compounds were tested for antitumor activity,and the results reveal that the methylglycine-substituted uridine compounds demonstrate a certain inhibitory effect on tumor growth,which lays an important foundation for the research of antitumor drugs.

关 键 词：氨基酸甲酯 尿苷 合成 抗肿瘤活性 

分 类 号：O626[理学—有机化学]