Biopolymers and cell. 2005; 21 (5): 433 - 439

he N1-glycosilic analogues of 6-azacytidine. Cytotoxic effect and influence on transcription in vitro

L. G. Palchikovs'ka, L. V. Garmanchouk, I. V. Alexeeva, L. S. Usenko, T. S. Shestakova, G. I. Solyanik, A. D. Shved, V. F. Chekhun

Cytotoxic action of the series of synthesized 6-azacytidine glycoside analogues in the range of 10^-2-10^-6 M on the tumor cell lines of epithelial origin has been studied. The most essential cytotoxic effect of 6-azaC analogues has been found for the MCF-7 cell line of the breast cancer. 6-Azacytosine xylofuranoside is the most effective among the compounds investigated. Index IC₅₀ for this compound is 0,63±0,01 mM and it is 4-7 times less than IC₅₀ for the other glycosides. The ability of analogues to modulate efficiency of model transcription system depending on the structure of glycosilyc fragment and concentration has been revealed.

Key words: 6-aza cytidine, 6-azacytosine glycosides, cytotoxic effect, tumor cell lines, the modelling system of a transcription, T7 RNA polymerase.