New insights regarding the potential of the pronucleotide approach in antiviral chemotherapy.

  • G Gosselin Laboratoire de Chimie Bioorganique, URA CNRS 488, Université de Montpellier II, France.;
  • J L Girardet
  • C Périgaud
  • S Benzaria
  • I Lefebvre
  • N Schlienger
  • A Pompon
  • J L Imbach

Abstract

The rationale for a pronucleotide approach based on the use of phosphotriesters which incorporate enzyme-mediated bio-labile protection is discussed in detail. Among the studied bio-labile phosphate protecting groups, the S-acyl-2-thioethyl (SATE) groups appeared the most promising as exemplified in cell culture systems in the case of the pronucleotides of 3'-azido-3'-deoxythymidine, 2',3'-didehydro-3'-deoxythymidine, 2',3'-dideoxyadenosine and acyclovir In vivo implementations of such bis(SATE) pronucleotides have been planned for future animal studies.
Published
1996-03-31
Section
Articles