1.
Eur J Med Chem
; 36(10): 771-82, 2001 Oct.
Artículo
en Inglés
| MEDLINE
| ID: mdl-11738485
RESUMEN
Several new 1,2,5-oxadiazole N-oxide derivatives and some deoxygenated analogues were synthesized to be tested as potential selective hypoxic cell cytotoxins. Compounds prepared were designed in order to gain insight into the mechanism of action of this kind of cytotoxin. Compounds were tested in oxia and hypoxia and they proved to be non-selective. 3-Cyano-N(2)-oxide-4-phenyl-1,2,5-oxadiazole showed the best cytotoxic activity in oxia. The cytotoxicity observed for these derivatives could be explained in terms of the electronic characteristics of the 1,2,5-oxadiazole substituents. Electrochemical and ESR studies were performed on the more cytotoxic derivative.
Asunto(s)
Antineoplásicos/síntesis química , Oxadiazoles/química , Oxadiazoles/síntesis química , Aerobiosis/fisiología , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Hipoxia de la Célula/fisiología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Células Clonales , Cricetinae , Citotoxinas/farmacología , Relación Estructura-Actividad
2.
J Pharm Sci
; 71(12): 1406-8, 1982 Dec.
Artículo
en Inglés
| MEDLINE
| ID: mdl-7153893