1. Academic Validation
  2. Anti-HIV pronucleotides: decomposition pathways and correlation with biological activities

Anti-HIV pronucleotides: decomposition pathways and correlation with biological activities

  • Bioorg Med Chem Lett. 1998 May 5;8(9):1045-50. doi: 10.1016/s0960-894x(98)00158-9.
D Egron 1 I Lefebvre C Périgaud T Beltran A Pompon G Gosselin A M Aubertin J L Imbach
Affiliations

Affiliation

  • 1 Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, France.
Abstract

The purpose of the present study was to compare the decomposition pathways in CEM cell extracts of various phenyl phosphoramidate derivatives of AZT. In addition, the structures of their metabolites were identified. Correlations with their anti-HIV activities in a thymidine kinase deficient (TK-) CEM cell line have been established with a rationale of designing phosphoramidate pronucleotides capable of delivering intracellularly their respective 5'-nucleoside monophosphate derivatives.

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