Synthesis and structure activity relationships of 5-substituted-4′-thio-β-D-arabinofuranosylcytosines

Academic Article


  • Four 5-substituted (chloro, fluoro, bromo, methyl) 1-(4-thio-β-D-arabinofuranosyl) cytosines and their α anomers were synthesized by a facile route in high yields. All of these nucleosides were evaluated for cytotoxicity against a panel of human tumor cell lines in vitro. Only 5-fluoro-1-(4-thio-β-D-arabinofuranosyl)cytosine was found to be highly cytotoxic in all the cell lines and was further evaluated in vivo.
  • Digital Object Identifier (doi)

    Author List

  • Tiwari KN; Shortnacy-Fowler AT; Cappellacci L; Waud WR; Parker WB; Montgomery JA; Secrist JA
  • Start Page

  • 2005
  • End Page

  • 2017
  • Volume

  • 19
  • Issue

  • 10-12