Design and synthesis of cADPR analogues with simplified ribose and nucleobase  

醚链和碳链修饰的cADPR类似物的设计合成及活性研究(英文)

作　　者：周玥[1] 余沛霖[1] 杨振军[1] 张亮仁[1] 张礼和[1] 

机构地区：[1]北京大学医学部天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2012年第4期287-291,共5页中国药学（英文版）

基　　金：National Natural Sciences Foundation of China (Grant No. 90713005,20910094);the Ministry of Education of China (Grant No. 200800010078)

摘　　要：New cADPR mimic 5 that integrates the simplified nucleobase and ribose was designed and synthesized by using Cu（I）-catalyzed Huisgen [3＋2] cycloaddition to build the simplified triazole nucleobase and microwave-assisted reaction to carry out intramolecular pyrophosphorylation. Primary biological investigation showed that the introduction of an ether strand to replace northern and southern riboses could retain calcium inducing activity, but the introduction of a carbon strand to replace the northern ribose could lead to decreased activity.设计并合成了一类新型的碱基与糖环简化的cADPR类似物。该化合物通过Cu(I)催化的Huisgen环加成反应构建三氮唑碱基, 并采用微波辅助法完成分子内的环合反应。初步的生物活性结果表明北区和南区糖环如果用醚链替换可保持化合物活性, 而北区糖环如果用碳链替换则会导致活性消失。

关 键 词：CADPR Click chemistry Microwave-assistance Synthesis 

分 类 号：R914[医药卫生—药物化学]