Rational design of a new series of pronucleotide

  • Bioorg Med Chem Lett. 2001 Jul 9;11(13):1775-7. doi: 10.1016/s0960-894x(01)00299-2.
T Beltran  1 ,  D Egron ,  A Pompon ,  I Lefebvre ,  C Périgaud ,  G Gosselin ,  A Aubertin ,  J Imbach
Affiliations
  • 1. UMR 5625 CNRS-UM II, Université Montpellier II, cc 008, place E. Bataillon, 34095 Cedex 05, Montpellier, France.
PMID: 11425558 DOI: 10.1016/s0960-894x(01)00299-2
Abstract

A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in TK(-) cell line, which proves 5'-AZTMP delivery.