Enhanced Cancer Cell Growth Inhibition by Dipeptide Prodrugs of Floxuridine: Increased Transporter Affinity and Metabolic Stability

@inproceedings{Tsume2008EnhancedCC,
  title={Enhanced Cancer Cell Growth Inhibition by Dipeptide Prodrugs of Floxuridine: Increased Transporter Affinity and Metabolic Stability},
  author={Yasuhiro Tsume and John M. Hilfinger and Gordon L Amidon},
  booktitle={Molecular pharmaceutics},
  year={2008}
}
  • Yasuhiro Tsume, John M. Hilfinger, Gordon L Amidon
  • Published in Molecular pharmaceutics 2008
  • Chemistry, Medicine
  • Dipeptide monoester prodrugs of floxuridine were synthesized, and their chemical stability in buffers, resistance to glycosidic bond metabolism, affinity for PEPT1, enzymatic activation and permeability in cancer cells were determined and compared to those of mono amino acid monoester floxuridine prodrugs. Prodrugs containing glycyl moieties were the least stable in pH 7.4 buffer ( t 1/2 < 100 min). The activation of all floxuridine prodrugs was 2- to 30-fold faster in cell homogenates than… CONTINUE READING

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