嘧啶衍生物对牛蒡子苷元片段修饰的研究有机化学.pdfVIP

DOI: 10.6023/cjoc201203001 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 嘧啶衍生物对牛蒡子苷元片段修饰的研究 王欢欢a 吴 平a 康 宏b 许 亮a 朱瑞新*,a,b 康廷国*,a (a 辽宁中医药大学药学院 大连 116600) (b 同济大学生命科学与技术学院 上海 200092) 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 1 物, 通过 H 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. 关键词 牛蒡子苷元; 结构修饰; 嘧啶衍生物; 异分子孪生药物 Modify a Fragment of Arctigenin with Pyrimidine Derivatives Wang, Huanhuana Wu, Pinga Kang, Hongb Xu, Lianga Zhu, Ruixin*,a,b Kang, Tingguo*,a a ( School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600) b ( School of Life Sciences and Technology, Tongji University, Shanghai 200092) Abstract 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 1H 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-