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- Title
Electron-Affinic SensitizationVII. A Correlation between Structures, One-Electron Reduction Potentials, and Efficiencies of Nitroimidazoles as Hypoxic Cell Radiosensitizers.
- Authors
Adams, G. E.; Flockhart, I. R.; Smithen, C. E.; Stratford, I. J.; Wardman, P.; Watts, M. E.
- Abstract
Radiosensitization efficiencies for seven different 2-nitroimidazoles including Ro-07-0582 and its urinary metabolite, Ro-05-9963, and two 5-nitroimidazoles including metronidazole, have been determined in hypoxic Chinese Hamster cells, line V79-379A, X-irradiated in vitro. All the compounds were active hypoxic cell sensitizers with the enhancement ratios increasing with drug concentration. The 2-nitroimidazoles were all more efficient than the 5-nitroimidazoles. Overall, the efficiencies, defined as the concentration required to give a particular enhancement ratio, varied by a factor of about 200. Electron-affinities of the sensitizers were determined by pulse radiolysis as the one-electron reduction potentials and these correlate well with the sensitization efficiencies of the compounds. The correlation extends beyond the nitroimidazole series as is shown by data for p-nitroacetophenone, nifuroxime (a nitrofuran) and oxygen itself. The nitroimidazoles varied by a factor of 70 in their octanol/water partition coefficients, but the effect of this parameter on sensitizing efficiency is small compared with the influence of electron affinity.
- Subjects
SINGLE electron transfer mechanisms; NITROIMIDAZOLES; DRUG efficacy; RADIATION-sensitizing agents; HAMSTERS as laboratory animals; THERAPEUTICS
- Publication
Radiation Research, 2012, Vol 178, Issue 2, pAV183
- ISSN
0033-7587
- Publication type
Article
- DOI
10.1667/RRAV14.1