Pulse radiolysis and cellular studies of a new class of radiosensitizers: 2-nitrobenzofurans.
AffiliationPaterson Laboratories, Christie Hospital and Holt Radium Institute, Withington, Manchester, M20 9BX, UK
MetadataShow full item record
AbstractA group of 2-nitrobenzofurans possessing antibacterial and antiparasitic properties have now been shown to be potential radiosensitizers from investigations in simple aqueous solution by pulse radiolysis and from survival studies in yeast. The radical anions of several 2-nitrobenzofurans were formed by the rapid reaction of the parent molecules with hydrated electrons or with various pyrimidine electron adducts. Studies of equilibria between these radical anions, the parent nitrobenzofurans and the corresponding species derived from quinones with known one-electron reduction potentials, showed that the one-electron reduction potentials of all the furans under investigation lie between -285 and -309 mV. They are thus more electron affinic than the nitroimidazoles (misonidazole and metronidazole) currently under clinical evaluation. 5-Hydroxy- and 7-hydroxy-2-nitrobenzofuran were demonstrated to form weak complexes with DNA (binding constant 80 M-1) and strong complexes with HSA (binding constant 10(5)M-1). In the yeast Saccharomyces cerevisiae the nitrobenzofurans exert radiosensitizing effects on survival either similar to or higher than misonidazole.
CitationPulse radiolysis and cellular studies of a new class of radiosensitizers: 2-nitrobenzofurans. 1982, 42 (4):457-68 Int. J Radiat Biol Relat Stud Phys Chem Med
JournalInternational Journal of Radiation Biology and Related Studies in Physics, Chemistry, and Medicine
- Electron-affinic sensitization. VII. A correlation between structures, one-electron reduction potentials, and efficiencies of nitroimidazoles as hypoxic cell radiosensitizers.
- Authors: Adams GE, Flockhart IR, Smithen CE, Stratford IJ, Wardman P, Watts ME
- Issue date: 1976 Jul
- Some examples of anomalous radiosensitizing behaviour of electron-affinic compounds in vitro.
- Authors: Watts ME, Jacobs RS
- Issue date: 1978 Jun
- Radiation-induced hydroxylation of thymine promoted by electron-affinic compounds.
- Authors: Nishimoto S, Ide H, Wada T, Kagiya T
- Issue date: 1983 Dec
- [Interaction of electron acceptor radiosensitizers with cell reducing systems].
- Authors: Basenova AT, Voronina SS, Balmukhanov BS
- Issue date: 1982 Nov-Dec
- The nitroimidazoles as radiosensitizers and cytotoxic agents.
- Authors: Hall EJ, Miller R, Astro M, Rini F
- Issue date: 1978 Jun