Potentiation of melphalan activity against a murine tumour by nitroimidazole compounds.
Br J Cancer
; 46(4): 525-31, 1982 Oct.
Article
en En
| MEDLINE
| ID: mdl-7138761
The activity against murine anaplastic MT tumours of the chemotherapeutic agent melphalan, either alone or in combination with one of 6 nitroimidazole compounds, was assayed using an in vivo-in vitro tumour excision assay. The melphalan alone proved cytotoxic to the tumour, whereas relatively little cytotoxicity was produced by any of the nitroimidazoles alone. When the nitroimidazole were given in combination with melphalan, dose-modifying potentiation of its cytotoxicity was observed. Maximum potentiation occurred when the nitroimidazoles were given 0--30 min before the melphalan, although some potentiation was still evident when they were given up to 2 h before or after. There was no threshold in nitroimidazole dose required to produce this potentiation, the degree of potentiation increasing with dose, albeit at a diminishing rate, to give maximum dose-modification factors of about 3. The 6 nitroimidazole compounds in order of increasing effectiveness as potentiators of melphalan activity were: METRO, Ro 05-9963, MISO, RSU 1047, Ro 03-8800 and Ro 03-8799. This order corresponds to the increasing electron affinity of these compounds. The most effective compound here, Ro 03-8799, was about twice as effective as the most widely used nitroimidazole in such studies, MISO.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Melfalán
/
Neoplasias Experimentales
/
Nitroimidazoles
Límite:
Animals
Idioma:
En
Revista:
Br J Cancer
Año:
1982
Tipo del documento:
Article
Pais de publicación:
Reino Unido