Sugar-modified derivatives of cytostatic 7-(het)aryl-7-deazaadenosines: 2 '-C-methylribonucleosides, 2 '-deoxy-2 '-fluoroarabinonucleosides, arabinonucleosides and 2 '-deoxyribonucleosides
2012
Abstract
A series of novel sugar-modified derivatives of cytostatic 7-hetaryl-7-deazaadenosines (2'-C-methylribonucleosides, 2'-deoxy-2'-fluoroarabinonucleosides, arabinonucleosides and 2'-deoxyribonucleosides) was prepared and screened for biological activity. Several examples of 2'-C-Me-ribonucleosides showed moderate anti-HCV activities in a replicon assay accompanied by cytotoxicity.
Several 7-hetaryl-7-deazaadenine fluoroarabino- and arabinonucleosides exerted moderate micromolar cytostatic effects. However, all the sugar-modified derivatives were less active than the parent ribonucleosides.