SATE Pronucleotide Approaches: An Overview

S.      Peyrottes; D.      Egron; I.      Lefebvre; G.      Gosselin; J.-   L.   Imbach; C.      Perigaud

doi:10.2174/1389557043404007

Abstract

This review depicts in vitro and in vivo results obtained with nucleotide prodrugs (pronucleotides) bearing S-acyl-2-thioethyl (SATE) groups as esterase-labile phosphate protections. New developments are illustrated by the design of mononucleoside mixed phosphoester derivatives leading to the selective intracellular delivery of the corresponding 5-mononucleotide through two different enzyme-mediated activation steps.

Keywords: nucleotide, prodrug, antiviral, phosphotriester, phosphoramidate, esterase, phosphoamidase, bioconversion

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Mini-Reviews in Medicinal Chemistry

Title: SATE Pronucleotide Approaches: An Overview

Volume: 4 Issue: 4

Author(s): S. Peyrottes, D. Egron, I. Lefebvre, G. Gosselin, J.- L. Imbach and C. Perigaud

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Keywords: nucleotide, prodrug, antiviral, phosphotriester, phosphoramidate, esterase, phosphoamidase, bioconversion

Abstract: This review depicts in vitro and in vivo results obtained with nucleotide prodrugs (pronucleotides) bearing S-acyl-2-thioethyl (SATE) groups as esterase-labile phosphate protections. New developments are illustrated by the design of mononucleoside mixed phosphoester derivatives leading to the selective intracellular delivery of the corresponding 5-mononucleotide through two different enzyme-mediated activation steps.

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Peyrottes S., Egron D., Lefebvre I., Gosselin G., Imbach L. J.- and Perigaud C., SATE Pronucleotide Approaches: An Overview, Mini-Reviews in Medicinal Chemistry 2004; 4 (4) . https://dx.doi.org/10.2174/1389557043404007