PMID: 6335498Dec 1, 1984

Thiol reactive nitroimidazoles: radiosensitization studies in vitro and in vivo

International Journal of Radiation Biology and Related Studies in Physics, Chemistry, and Medicine
I J StratfordP W Sheldon

Abstract

Using Chinese hamster V79 cells in vitro a study has been made of the radiosensitizing properties of 4- or 5-nitroimidazoles substituted in the 2, 5 or 4 position with various halo, sulphur ether, sulphonamide, sulphonate, ether or nitro groups. Values of E17 (the one-electron reduction potential measured versus the normal hydrogen electrode at pH7) vary in the range -178 to -565 mV. All the compounds, with one exception, are more efficient radiosensitizers than would be predicted from their redox potentials, and the factor, C1.6/C1.6, by which a compound is more efficient has been calculated. The second-order rate constants, k2, for reaction of these nitroimidazoles with glutathione and/or dithiothreitol were determined. Within each class of nitroimidazole there is a trend for k2 to increase with increasing redox potential. However, there is no clear trend between k2 and C1.6/C1.6. The concentration required to cause a 50 per cent depletion of intracellular glutathione was determined for selected compounds, as was the ability of glutathione-S-transferase to catalyse reaction with thiols. These observations suggested that the relative thiol reactivity measured under chemically controlled conditions does not necessarily indicate...Continue Reading

References

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Citations

Mar 1, 1993·International Journal of Hyperthermia : the Official Journal of European Society for Hyperthermic Oncology, North American Hyperthermia Group·M RybczynskaC Poyart
Jul 1, 1987·International Journal of Radiation Biology and Related Studies in Physics, Chemistry, and Medicine·J M WallingG E Adams
Jul 1, 1987·International Journal of Radiation Biology and Related Studies in Physics, Chemistry, and Medicine·P K ChanB R James
Jul 1, 1986·International Journal of Radiation Oncology, Biology, Physics·T J KinsellaA J Fornace
Jul 1, 1986·International Journal of Radiation Oncology, Biology, Physics·M E WattsPeter Wardman
Jul 1, 1986·International Journal of Radiation Oncology, Biology, Physics·J B MitchellA Russo
Apr 1, 1989·International Journal of Radiation Oncology, Biology, Physics·J M Brown

Related Concepts

Combined Modality Therapy
Cricetulus
Sputolysin
Reduced Glutathione
Cricetus
Neoplasms, Experimental
Nitroimidazoles
Radiation-Sensitizing Effect

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