Pulse radiolysis and cellular studies of a new class of radiosensitizers: 2-nitrobenzofurans.
Int J Radiat Biol Relat Stud Phys Chem Med
; 42(4): 457-68, 1982 Oct.
Article
en En
| MEDLINE
| ID: mdl-6757163
A 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.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fármacos Sensibilizantes a Radiaciones
/
Saccharomyces cerevisiae
/
Benzofuranos
/
Nitrofuranos
Idioma:
En
Revista:
Int J Radiat Biol Relat Stud Phys Chem Med
Año:
1982
Tipo del documento:
Article
Pais de publicación:
Reino Unido