Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Cytotoxicity and Pharmacokinetics of 1-β-D-Arabinofuranosyl-2-thiocytosine, a 2-Sulphur Substituted Derivative of Cytarabine
Takeo KAWAGUCHITomohisa ICHIKAWATetsuya HASEGAWAMineo SANEYOSHIAyako YUKITAMakoto ASANOToshiyuki WAKAYAMAHisatoyo KATOToshiyuki NAGATA
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1999 Volume 22 Issue 1 Pages 100-102

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Abstract

1-(β-D-Arabinofuranosyl)-2-thiocytosine (araSC), a 2-substituted derivative of cytarabine (araC), has been investigated for its cytotoxicity, enzymatic stability, plasma concentration-time profile in mice, and cytokinetics.This derivative showed strong cytotoxicity in several mammalian cell lines, although activity (IC50s) was weaker than araC. Greater stability to mouse cytidine deaminase was observed; the half-line in the presence of the enzyme was about 4-times longer than that of araC. The plasma concentration-time profile in mice in vivo showed prolonged retention of araSC when compared with araC. Cytokinetic study using flow cytometry indicated a non-S-phase specific effect of this compound.

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