Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy.

@article{Rossiter2002HalogenatedIA,
  title={Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy.},
  author={Sharon Rossiter and Lisa K. Folkes and Peter Wardman},
  journal={Bioorganic & medicinal chemistry letters},
  year={2002},
  volume={12 18},
  pages={2523-6}
}
Substituted indole-3-acetic acid (IAA) derivatives, plant auxins with potential for use as prodrugs in enzyme-prodrug directed cancer therapies, were oxidised with horseradish peroxidase (HRP) and toxicity against V79 Chinese hamster lung fibroblasts was determined. Rate constants for oxidation by HRP compound I were also measured. Halogenated IAAs were found to be the most cytotoxic, with typical surviving fractions of <10(-3) after incubation for 2h with 100 microM prodrug and HRP.