新型核苷和单糖1,2,3-三唑寡聚缀合物的合成及抗肿瘤活性  

Synthesis and Antitumor Activities of Novel 1,2,3-Triazolefused Oligoconjugates Based on Nucleoside and Saccharide

作　　者：金培元[1] 卢金荣[1] 赵长琦[2] 巨勇[1,3] 

机构地区：[1]清华大学化学系生命有机磷化学及化学生物学教育部重点实验室,北京100084 [2]北京师范大学生命科学学院,北京100875 [3]兰州大学功能有机分子化学国家重点实验室,兰州730000

出　　处：《有机化学》2012年第9期1673-1677,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21172130);国家重点基础研究发展规划(973计划)(No.2012CB821600)资助项目~~

摘　　要：利用"点击反应"合成了一系列核苷和单糖的1,2,3-三唑寡聚缀合物7～12,其结构经1H NMR,MS确认.对所合成化合物进行了抑制Hela宫颈癌细胞增殖的体外活性筛选,发现二(脱氧胸苷)乙二醚三唑缀合物11a具有较好的抑制活性,且明显优于其核苷母体3'-叠氮-3'-脱氧胸苷.Novel 1,2,3-triazole-fused oligoconjugates 7-12 based on nucleoside and saecharide were synthesized via click chemistry. The structures were confirmed by 1H NMR and MS, and their antitumor activities were assayed against cervix can- cer HeLa cells in vitro. The preliminary bioassay test shows that only bis（triazole） nucleoside 11a considerably inhibited the growth of cervix cancer HeLa cells and was much better than azidothymidine.

关 键 词：寡聚 缀合物 点击化学 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] O633.5[医药卫生—药学]