Konč Juraj, Tichý Michal, Pohl Radek, Hodek Jan, Džubák Petr, Hajdúch Marián, Hocek Michal
Institute of Organic Chemistry and Biochemistry , Czech Academy of Sciences , Flemingovo nam. 2 , CZ-16610 Prague 6 , Czech Republic . Email:
Institute of Molecular and Translational Medicine , Palacky University and University Hospital in Olomouc , Faculty of Medicine and Dentistry , Hněvotínská 5 , CZ-775 15 Olomouc , Czech Republic.
Medchemcomm. 2017 Aug 25;8(9):1856-1862. doi: 10.1039/c7md00319f. eCollection 2017 Sep 1.
Three types of sugar modified pyrimido[4,5-]indole nucleosides (2'-deoxy-2'-fluororibo-, 2'-deoxy-2'-fluoroarabino- and arabinonucleosides) were synthesized by glycosylation of 4,6-dichloropyrimido[4,5-]indole followed by modification of sugar moiety and introduction of substituents into position 4 by cross-coupling reactions or nucleophilic substitutions. Some 2'-fluororibo- and 2'-fluoroarabinonucleosides displayed interesting anti-HCV activities (IC = 1.6-20 μM) and the latter compounds also some anti-dengue activities (IC = 10.8-40 μM).
通过4,6-二氯嘧啶并[4,5-]吲哚的糖基化反应，随后对糖部分进行修饰，并通过交叉偶联反应或亲核取代反应在4位引入取代基，合成了三种糖修饰的嘧啶并[4,5-]吲哚核苷（2'-脱氧-2'-氟核糖核苷、2'-脱氧-2'-氟阿拉伯糖核苷和阿拉伯糖核苷）。一些2'-氟核糖核苷和2'-氟阿拉伯糖核苷表现出有趣的抗丙型肝炎病毒活性（IC = 1.6 - 20 μM），后一类化合物还具有一些抗登革热活性（IC = 10.8 - 40 μM）。
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