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Title: 6-[2-phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines: a new class of acyclic pyrimidine nucleoside phosphonates with antiviral activity
Authors: Balzarini, Jan ×
Pannecouque, Christophe
Naesens, Lieve
Andrei, Graciela
Snoeck, Robert
De Clercq, Erik
Hocková, D
Holý, A #
Issue Date: Oct-2004
Publisher: Marcel Dekker
Series Title: Nucleosides, Nucleotides & Nucleic Acids vol:23 issue:8-9 pages:1321-1327
Conference: Joint 9th European/11th International Meeting on Purines and Pyrimidines location:Amsterdam, The Netherlands date:2003
Abstract: Acyclic nucleoside phosphonate derivatives containing a pyrimidine base preferably bearing amino groups at C-2 and C-4 (DAPym), and linked at the C-6 position to (S)-[3-hydroxy-2-(phosphonomethoxy)propoxy] (HPMPO), 2-(phosphonomethoxy) ethoxy (PMEO) or (R)-[2-(phosphonomethoxy)propoxy] (PMPO), display an antiviral sensitivity spectrum that closely mimic that of the parental (S)-HPMP-, PME- and (R)-PMP-purine derivatives. Several PMEO-DAPym derivatives proved as potent as PMEA (adefovir) and (R)-PMPA (tenofovir) in inhibiting Moloney murine sarcoma virus (MSV)-induced tumor formation in newborn NMRI mice. The HPMPO-, PMEO- and PMPO-DAPym derivatives represent a novel well-defined subclass among the acyclic nucleoside phosphonates endowed with potent and selective antiviral activity.
ISSN: 1525-7770
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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