Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy.

@article{Davies2005NovelFP,
  title={Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy.},
  author={Lawrence C Davies and Frank Friedlos and Douglas D. Hedley and Jan M. L. Martin and Lesley M Ogilvie and Ian J Scanlon and Caroline Joy Springer},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 16},
  pages={
          5321-8
        }
}
Sixteen novel polyfluorinated benzoic acid mustards have been synthesized for use in gene-directed enzyme prodrug therapy (GDEPT). Eight of these were benzoic acid L-glutamate mustards for evaluation as prodrugs and the other eight were the active drugs formed by the action of the bacterial enzyme carboxypeptidase G2 (CPG2). All of the di- and trifluorinated prodrugs were efficiently cleaved by the enzyme. In contrast, the tetrafluorinated prodrugs were found to be competitive inhibitors of… CONTINUE READING
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