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Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy
Sharon Rossiter1, Lisa K Folkes, Peter Wardman
1Gray Cancer Institute, PO Box 100, Mount Vernon Hospital, Northwood, HA6 2JR, Middlesex, UK. s.rossiter@ucl.ac.uk
Bioorganic & Medicinal Chemistry Letters
|August 17, 2002
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.