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Title: Anti-retroviral and cytostatic activity of 2',3'-dideoxyribonucleoside 3'-disulfides
Authors: Gerland, Béatrice ×
Désiré, Jérôme
Balzarini, Jan
Décout, Jean-Luc #
Issue Date: Jul-2008
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:16 issue:14 pages:6824-6831
Abstract: Herein, we report the synthesis, antiviral and cytostatic effects of nucleosides bearing a 3'-disulfide function as prodrugs of potentially active 3'-mercaptonucleotides. The lack of the anti-HIV effects in mutant CEM/TK-cells for most of the thymidine disulfides suggests that a phosphorylation step involving thymidine kinase is necessary for the eventual antiviral activity of the thymidine nucleosides. The comparable anti-HIV activities of most of the disulfides and their rapid reduction in CEM cell extracts imply an inhibitory effect of the 2',3'-dideoxy-3'-mercaptothymidine 5'-triphosphate metabolite. The cytostatic effects of the disulfides in CEM/0 and Molt4/C8 cells appeared to be strongly dependent on the nature of the non-nucleosidic disulfide moiety and were decreased in preserving the anti-retroviral activity.
URI: 
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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