嘧啶衍生物对牛蒡子苷元片段修饰的研究  

Modify a Fragment of Arctigenin with Pyrimidine Derivatives

作　　者：王欢欢[1] 吴平[1] 康宏[2] 许亮[1] 朱瑞新[1,2] 康廷国[1] 

机构地区：[1]辽宁中医药大学药学院,大连116600 [2]同济大学生命科学与技术学院,上海200092

出　　处：《有机化学》2012年第10期1894-1898,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.30976611);中国高等教育博士研究基金计划(No.20100072120050);上海中药现代化(No.09dZ1972800)资助项目~~

摘　　要：用一系列具有生物活性的嘧啶衍生物修饰牛蒡子苷元,旨在寻找增强牛蒡苷元子抗肿瘤活性的同时又能降低嘧啶抗肿瘤副作用的先导化合物.本研究通过把卤代后的嘧啶衍生物与牛蒡子苷元酚羟基相接,合成得到11个新的化合物,通过1H NMR与LC-MS表征确定其结构.最终,增加了牛蒡子苷元抗肿瘤化合物库中化合物的数量,为接下来的体外活性筛选做准备.In order to enhance the anti-tumor activity of the arctigenin and reduce the side effects of pyrimidine, arctigenin was modified with pyrimidine derivatives having biological activities. In this research, some halogenated pyrimidines were linked to the phenolic hydroxyl group of the arctigenin to gain eleven new compounds, and the structures of them were identi- fied by LC-MS and IH NMR. So, the number of the anti-tumor compound libraries of compounds based on arctigenin was increased, and these compounds were prepared for the in-vitro activity screening in the near future. By our work, when en- hance the alkalinity and increase the water content in DMF, the etherification reaction is promoted, to a certain extent.

关 键 词：牛蒡子苷元 结构修饰 嘧啶衍生物 异分子孪生药物 

分 类 号：O626.41[理学—有机化学]