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

M Quintiliani, L Persoons, N Solaroli, A Karlsson…

Index: Quintiliani, Maurizio; Persoons, Leentje; Solaroli, Nicola; Karlsson, Anna; Andrei, Graciela; Snoeck, Robert; Balzarini, Jan; McGuigan, Christopher Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 14 p. 4338 - 4345

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Citation Number: 5

Abstract

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 ...