1. Effect of catechol derivatives on cell growth and lipoxygenase activity.
- Author
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Simpson J, Forrester R, Tisdale MJ, Billington DC, and Rathbone DL
- Subjects
- Animals, Arachidonate 12-Lipoxygenase metabolism, Arachidonate 15-Lipoxygenase metabolism, Arachidonic Acid metabolism, Cell Division drug effects, Cell Line, Tumor, Indicators and Reagents, Mice, Molecular Conformation, Rabbits, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Catechols chemical synthesis, Catechols pharmacology, Lipoxygenase Inhibitors chemical synthesis, Lipoxygenase Inhibitors pharmacology
- Abstract
Derivatives of salicylic acid have been synthesized as potential lipoxygenase inhibitors. Agents containing a phenolic dihydroxy moiety showed potent (IC(50)10(-6)-10(-7) M) inhibition of the growth of murine colonic tumour cells in vitro, and were effective inhibitors of 5-, 12- and 15-lipoxygenase in intact cells. The catechols were also potent inhibitors of rabbit reticulocyte 15-lipoxygenase (IC(50) approximately 1 microM).
- Published
- 2003
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