Synthesis and Biological Activity of 5-Fluoro-2-thiocytosine Nucleosides

M. Bretner Institute of Biochemistry and Biophysics, Polish Academy of Sciences, 5a Pawinskiego St., 02-106, Warszawa, Poland

M. Balinska Nencki Institute of Experimental Biology, Polish Academy of Sciences, 3 Pasteur St., Warszawa, Poland

K. Krawiec Institute of Biochemistry and Biophysics, Polish Academy of Sciences, 5a Pawinskiego St., 02-106, Warszawa, Poland

B. Kierdaszuk Institute of Experimental Physics, University of Warsaw, 93 Zwirki i Wigury St., 02-089, Warszawa, Poland

D. Shugar Institute of Biochemistry and Biophysics, Polish Academy of Sciences, 5a Pawinskiego St., 02-106, Warszawa, Poland

T. Kulikowski Institute of Biochemistry and Biophysics, Polish Academy of Sciences, 5a Pawinskiego St., 02-106, Warszawa, Poland

Abstract

Two pathways are described for the synthesis of the 2′-deoxynucleosides of 2-thiocytosine and 5-fluoro-2-thiocytosine: (a) by nucleoside condensation, (b) by amination of the corresponding nucleosides of 2,4-dithiouracil. Biological activities vs two cell systems are described. The nucleosides are moderate to weak substrates of deoxycytidine kinase and, partly as a result of this, reasonable good inhibitors of the enzyme

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Synthesis and Biological Activity of 5-Fluoro-2-thiocytosine Nucleosides

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Synthesis and Biological Activity of 5-Fluoro-2-thiocytosine Nucleosides

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