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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology*
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Cell Line
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Cricetinae
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Halogens / chemistry*
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Horseradish Peroxidase / metabolism
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Indoleacetic Acids / chemistry*
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Indoleacetic Acids / metabolism
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Indoleacetic Acids / pharmacology*
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Kinetics
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Oxidation-Reduction
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Prodrugs / chemistry*
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Prodrugs / metabolism
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Prodrugs / pharmacology*
Substances
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Antineoplastic Agents
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Halogens
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Indoleacetic Acids
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Prodrugs
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indoleacetic acid
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Horseradish Peroxidase