Title: Rapid microwave-enhanced synthesis of C5-alkynyl pyranonucleosides as novel cytotoxic antitumor agents
Authors: Dimopoulou, Athina ×
Manta, Stella
Kiritsis, Christos
Gkaragkouni, Dimitra-Niki
Papasotiriou, Ioannis
Balzarini, Jan
Komiotis, Dimitri #
Issue Date: Mar-2013
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:23 issue:5 pages:1330-3
Article number: 10.1016/j.bmcl.2012.12.092
Abstract: A microwave-assisted, one-pot, coupling reaction for the synthesis of C5-alkynyl-uracil and cytosine glucopyranonucleosides has been developed. The reaction is carried out under standard Sonogashira coupling conditions from glucopyranonucleosides of 5-iodouracil or 5-iodocytosine and various terminal alkynes. All compounds were evaluated for their cytostatic and antiviral activity. The 5-phenylethynyluracil pyranonucleoside derivative 6a showed the most promising cytostatic activity (50% inhibitory concentration in the lower micromolar range). No meaningful antiviral activity was recorded.
ISSN: 0960-894X
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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