2. Academic Validation
  3. Design, synthesis and biological evaluation of 2'-deoxy-2',2'-difluoro-5-halouridine phosphoramidate ProTides

Design, synthesis and biological evaluation of 2'-deoxy-2',2'-difluoro-5-halouridine phosphoramidate ProTides

  • Bioorg Med Chem. 2011 Jul 15;19(14):4338-45. doi: 10.1016/j.bmc.2011.05.037.
Maurizio Quintiliani 1,  Leentje Persoons,  Nicola Solaroli,  Anna Karlsson,  Graciela Andrei,  Robert Snoeck,  Jan Balzarini,  Christopher McGuigan
Affiliations

Affiliation

  • 1 Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.
PMID: 21696963 DOI: 10.1016/j.bmc.2011.05.037
Abstract

We report the synthesis of a series of novel 2'-deoxy-2',2'-difluoro-5-halouridines and their corresponding phosphoramidate ProTides. All compounds were evaluated for Antiviral activity and for cellular toxicity. Interestingly, 2'-deoxy-2',2'-difluoro-5-iodo- and -5-bromo-uridines showed selective activity against feline herpes virus replication in Cell Culture due to a specific recognition (activation) by the virus-encoded thymidine kinase.

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