Abstract
We describe here the design, synthesis, and biological evaluation of H2O2-activatable nucleosides via an efficient and regioselective functionalization of unprotected precursors. Biological evaluation of a H2O2-specific responsive prodrug of gemecitabin demonstrates an extremely fast activation, low toxicity and enhanced anticancer effects in two cell lines.
MeSH terms
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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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Cell Line, Tumor
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Cell Membrane Permeability / drug effects
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Cell Survival / drug effects
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Deoxycytidine / analogs & derivatives
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Deoxycytidine / chemistry
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Drug Design
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Gemcitabine
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Humans
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Hydrogen Peroxide / chemistry*
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Nucleosides / chemical synthesis
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Nucleosides / chemistry*
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Nucleosides / pharmacology
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Prodrugs / chemical synthesis
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Prodrugs / chemistry
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Prodrugs / pharmacology
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Stereoisomerism
Substances
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Antineoplastic Agents
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Nucleosides
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Prodrugs
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Deoxycytidine
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Hydrogen Peroxide
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Gemcitabine