Biopolymers and cell. 2005; 21 (2): 174 - 179

5-Aminosubstituted triazine nucleosides and their furanidylic analogues: synthesis and primary screening on tumor cell models

I. V. Alexeeva, L. G. Palchikovs'ka, L. S. Usenko, V. G. Kostina

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.

Key words: 6-azacytidine, the triazine nucleosides, synthesis, structure, mitotic activity.