Biopolym. Cell. 1997; 13(4):285-290.
Structure and Function of Biopolymers
N4-deriva tives of 6-azacytidine: synthesis and biological activity
1Alexeeva I. V., 1Palchikovskaya L. I., 1Shalamay A. S., 1Tarnavsky S. S., 2Nosach L. M., 2Zhiovnovataya V. I., 2Dyachenko N. S.
  1. Institute of Molecular Biology and Genetics, NAS of Ukraine
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03680
  2. D. K. Zabolotny Institute of Microbiology and Virology, NAS of Ukraine
    154, Academika Zabolotnogo Str., Kyiv, Ukraine, 03680


Different methods of the synthesis of N4-derivatives of 6-azacytidine in conditions of simplified "sililic condensation" methods were investigated. Their antivirus activity with respect to the serotype 2 adenovirus in the culture of Hep-2 cells was studied. Primary specific activity of the compounds obtained was defined. Correlation between chemical structure of the new 6-azacytidine derivatives and its biological properties is discussed.


[1] Nosach LN, Diachenko NS, Butenko SI et al. Effect of 6-azacytidine for expression adenoviral genome. New approaches to chemotherapy of viral infections. Riga: Zinatne, 1991: 87-93.
[2] Nosach LN, Dyachenko NS, Shalamay AS, Alekseeva IV, Kushko LYa, Ozvinchuk II, Zhovnovataya VL, Butenko SL, Petrovskaya IA, Drannik GN. Antiadenovirus and immunostimulating actions of 6-azacylidine. Biopolym Cell. 1996; 12(1):75-85.
[3] Petrusha NA. [Toxico-pharmacological properties of 6-azacytidine]. Farmakol Toksikol. 1987;50(2):75-6.
[4] Levenko BA, Semenyuk DV, Kunakh VA et al. The study of the effect of derivatives of 6-azacytidine on the growth of isolated plant tissues. Exper. plant genetics. Kiev: Naukova Dumka, 1982. 116 p.
[5] Chernetskiy VP. Synthesis antimetabolites nucleic acid metabolism and their use in chemotherapy molecular diseases. Vistnyk AN URSR. 1971;(8): 30-41.
[6] Alekseeva IV, Pal’chikovskaya LI, Shalamai AS, Ognyanik SS, Morgart NV, Petrusha NA. Synthesis of N1-substituted 6-azacytosines and their biological activity. Pharmaceutical Chemistry Journal. 1994;28(4):227–30.
[7] Cristescu C, Sitaru S. As-triazine derivatives with potential therapeutic action. XI. Thionation of 6-methylthio-as-triazine-3,5 (2H, 4H)-dione. Revue Roumaine Chimie. 1971; 16(1):135-41.
[8] Gordon A, Ford P. Sputnik Khimika. M.: Mir, 1976; 541 p.
[9] Ognyanik SS, Tarnavsky SS, Sikora LI, Alekseeva IV. Synthesis and spectroscopic study of 3-thio-6-alkylaminosubstituted 1,2,4-triazines-5. Ukr Khim Zh. 1988;54(11):1197-9.
[10] ?emli?ka J, ?orm F. Nucleic acids components and their analogues. LXI. The reaction of dimethylchloromethyleneammonium chloride with the 2',3',5'-tri-O-acyl derivatives of uridine and 6-azauridine; A new synthesis of 6-azacytidine. Coll Chech Chem Commun. 1965; 30(10):2052-67.
[11] Nosach LN, Diachenko NS. Cytopathology of adenovirus infection. Kiev: Naukova Dumka, 1982. 124 p.
[12] Galegov VA, Pushkarskaya NA, Leont'eva NA et al. The program is a pilot study of antiviral chemotherapy (anti-influenza) products and the criteria for their evaluation phase. Vopr Virusol. 1976;9(4):503-7.