2. Academic Validation
  3. Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription

Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription

  • J Med Chem. 2003 Jun 19;46(13):2565-8. doi: 10.1021/jm0256225.
Béatrice Roy 1,  Stéphane Chambert,  Michel Lepoivre,  Anne-Marie Aubertin,  Jan Balzarini,  Jean-Luc Décout
Affiliations

Affiliation

  • 1 Institut de Biochimie Biophysique Moléculaire et Cellulaire, UMR 8619 CNRS, Université de Paris Sud, F-91405 Orsay, France. [email protected]
PMID: 12801219 DOI: 10.1021/jm0256225
Abstract

Herein, we report the design, synthesis, and biological effects of nucleosides bearing a disulfide function on the sugar ring as prodrugs of potentially active mercaptonucleotides that can target ribonucleotide reductase or Reverse Transcriptase. We show that cytidine derivatives efficiently reduce dNTP pools in human CEM/SS cells and that 3'-deoxythymidin-3'-yl methyl disulfide is able to interfere with both cellular dNTP synthesis and HIV reverse transcription.

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