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ID: ALA1135317
Journal: Bioorg Med Chem Lett
Title: Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy.
Authors: Rossiter S, Folkes LK, Wardman P.
Abstract: 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.
CiteXplore: 12182852