Biopolym. Cell. 2005; 21(2):174-179.
Bioorganic Chemistry
5-Aminosubstituted triazine nucleosides and their furanidylic analogues: synthesis and primary screening on tumor cell models
1Alexeeva I. V., 1Palchikovs'ka L. G., 1Usenko L. S., 1Kostina V. G.
  1. Institute of Molecular Biology and Genetics, NAS of Ukraine
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03680

Abstract

A number of new N-substituted triazine nucleosides and their furanidyl analogues were synthesized using a simplified silyl con­densation method. The primary screening of these compounds at 10–4 M concentration on human tumor cell models revealed a cytostatic effect only for the epoxy derivative of 6-azacytidine. It was shown that nucleoside modification at aglycone exocyclic amino group or sugar residue substitution with tetrahydrofuran ring led to unexpected stimulation of the mitotic activity of the cells tested. The observed new type of biological action can be explained by the interaction of 5-aminosubstituted nucleosides and their furanidyl analogues with cellular targets other than those for 6-azacytidine.
Keywords: 6-azacytidine, the triazine nucleosides, synthesis, structure, mitotic activity

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