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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

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

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.[1]

References

  1. Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy. Rossiter, S., Folkes, L.K., Wardman, P. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
 
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