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.
Crown Copyright © 2011. Published by Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology*
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology*
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Cell Proliferation / drug effects
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Cells, Cultured
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Dose-Response Relationship, Drug
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Drug Design*
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Drug Screening Assays, Antitumor
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Floxuridine / analogs & derivatives*
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Floxuridine / chemical synthesis
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Floxuridine / chemistry
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Floxuridine / pharmacology
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Hepacivirus / drug effects*
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Humans
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Mice
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Microbial Sensitivity Tests
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Molecular Conformation
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Phosphoric Acids / chemical synthesis
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Phosphoric Acids / chemistry
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Phosphoric Acids / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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Amides
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Antineoplastic Agents
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Antiviral Agents
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Phosphoric Acids
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Floxuridine
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phosphoramidic acid