In vitro and in vivo radiosensitization by 2-nitroimidazoles more electron-affinic than misonidazole
Journal Article
·
· Int. J. Radiat. Oncol., Biol. Phys.; (United States)
- Stanford Univ., CA
A series of 5-substituted-methyl-2 nitroimidazoles, more electron-affinic than misonidazole (MISO), has been studied as potential hypoxic cell radiosensitizers. In vitro radiosensitization studies of these compounds showed equivalent or greater radiosensitization than MISO, while LD/sub 50/ studies of the compounds found them to be, in general, more toxic to Balb/c mice than MISO. Radiosensitization experiments in vivo with compounds SR-2537, SR-2515 and SR-2553 of acceptable toxicity were not able to sensitize the EMT6 tumor to x-irradiation after a single intraperitoneal injection. However, moderate sensitization was achieved when SR-2537 was administered i.v. Rapid metabolism of these more electron-affinic compounds was suggested as a possible case of the poor sensitization. However, when multiple i.v. injections of SR-2537 were given to maintain a constant drug level in the tumor, radiosensitization by this compound did not improve, suggesting that intact drug was either not reaching or was not penetrating the hypoxic cells.
- OSTI ID:
- 7065978
- Journal Information:
- Int. J. Radiat. Oncol., Biol. Phys.; (United States), Journal Name: Int. J. Radiat. Oncol., Biol. Phys.; (United States) Vol. 8:3/4; ISSN IOBPD
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
560111 -- Radiation Effects on Biochemicals-- In Vitro-- (-1987)
560114 -- Radiation Effects on Biochemicals-- In Animals-- (-1987)
560152* -- Radiation Effects on Animals-- Animals
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AFFINITY
ANIMALS
ANTINEOPLASTIC DRUGS
AZOLES
DOSES
DRUGS
ELECTROMAGNETIC RADIATION
EXPERIMENTAL NEOPLASMS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
IN VITRO
IN VIVO
IONIZING RADIATIONS
LETHAL DOSES
MAMMALS
MICE
MISONIDAZOLE
NITRO COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PHARMACOLOGY
RADIATIONS
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
RODENTS
VERTEBRATES
X RADIATION
560114 -- Radiation Effects on Biochemicals-- In Animals-- (-1987)
560152* -- Radiation Effects on Animals-- Animals
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AFFINITY
ANIMALS
ANTINEOPLASTIC DRUGS
AZOLES
DOSES
DRUGS
ELECTROMAGNETIC RADIATION
EXPERIMENTAL NEOPLASMS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
IN VITRO
IN VIVO
IONIZING RADIATIONS
LETHAL DOSES
MAMMALS
MICE
MISONIDAZOLE
NITRO COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PHARMACOLOGY
RADIATIONS
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
RODENTS
VERTEBRATES
X RADIATION