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Design of new mononucleotide prodrugs: aryl (SATE) phosphotriester derivatives.

Authors :
Peyrottes S
Schlienger N
Beltran T
Lefebvre I
Pompon A
Gosselin G
Aubertin AM
Imbach JL
Périgaud C
Source :
Nucleosides, nucleotides & nucleic acids [Nucleosides Nucleotides Nucleic Acids] 2001 Apr-Jul; Vol. 20 (4-7), pp. 315-21.
Publication Year :
2001

Abstract

Synthesis, biological activities and decomposition kinetics of novel phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-tButyl-2-thioethyl (tBuSATE) group and L-tyrosinyl residues are reported. All the derivatives appeared to be potent inhibitors of HIV-1 replication in various cell culture experiments. The proposed decomposition process of these mixed phosphotriesters may involve successively an esterase and then a phosphodiesterase activation.

Details

Language :
English
ISSN :
1525-7770
Volume :
20
Issue :
4-7
Database :
MEDLINE
Journal :
Nucleosides, nucleotides & nucleic acids
Publication Type :
Academic Journal
Accession number :
11563043
Full Text :
https://doi.org/10.1081/NCN-100002302