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Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
SATE (aryl) phosphotriester series. I. Synthesis and biological evaluation
S Peyrottes1, G Gosselin, A M Aubertin
1Laboratoire de Chimie Organique Biomoléculaire de Synthèse, Université Montpellier II, UMR 5625 CNRS, Montpellier, France. peyrottes@univ-montp2.fr
Abstract:
Synthesis and biological activities of several phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-pivaloyl-2-thioethyl (tBuSATE) group and aryl residues derived from L-tyrosine are reported. All compounds showed marked anti-HIV activity in thymidine kinase-deficient CEM cells demonstrating their ability to deliver intracellularly the parent 5'-mononucleotide.
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