Radiosensitization of hypoxic mammalian cells by dinitroimidazoles. [. gamma. rays; Chinese hamster cells (V-79-753-B)]

Journal Article · Fri Jun 01 04:00:00 EDT 1979 · Radiat. Res.; (United States)

DOI:https://doi.org/10.2307/3574978· OSTI ID:6187798

Agrawal, K C ^[1]; Millar, B C; Neta, P

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1. Tulane Univ., New Orleans, LA

New compounds of the nitro- and dinitroimidazole series have been developed as radiosensitizers which selectively sensitize hypoxic mammalian cells to the lethal effect of ionizing radiation. Three compounds, 2,4(5)-dinitroimidazole, 2,4-dinitroimidazole-1-ehtanol (KA161), and an imidazooxazole derivative, 2,3-dihydro-5-nitroimidazo-(2,1-b)oxazole (KA151), were tested for their ability to sensitize hypoxic Chinese hamster cells (V-79-753 B) in vitro. These agents were also tested for their toxicity by exposing the Chinese hamster cells at 20/sup 0/C for 2 hr at various concentrations; the 2,4(5)-dinitroimidazole did not show toxicity up to mM concentration, whereas its 1-hydroxyethyly analog and KA151 were toxic to these cells at concentrations of 1 mM or higher. All the compounds were active sensitizers, 2,4-dinitroimidazole-t-ethanol (KA161) was the most effective radiosensitizer producing an enhancement ratio of 2.0 at 100 ..mu..m concentration and was found to be more efficient than misonidazole at this concentration. ESR studies of the radical anions indicated that KA161 also possessed a higher electron affinity than misonidazole.

• OSTI ID: 6187798
• Journal Information: Radiat. Res.; (United States), Journal Name: Radiat. Res.; (United States) Vol. 78:3; ISSN RAREA
• Country of Publication: United States
• Language: English

Related Subjects

560121* -- Radiation Effects on Cells-- External Source-- (-1987)
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMAL CELLS
ANOXIA
AZOLES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL EFFECTS
BIOLOGICAL RADIATION EFFECTS
CELL CULTURES
COBALT 60
COBALT ISOTOPES
COMPARATIVE EVALUATIONS
DATA
DATA FORMS
DRUGS
ELECTROMAGNETIC RADIATION
EXPERIMENTAL DATA
GAMMA RADIATION
GRAPHS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
IN VITRO
INFORMATION
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
IONIZING RADIATIONS
IRRADIATION
ISOLATED VALUES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
MINUTES LIVING RADIOISOTOPES
NITRO COMPOUNDS
NUCLEI
NUMERICAL DATA
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIATION EFFECTS
RADIATIONS
RADIOISOTOPES
RADIOSENSITIVITY
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
RESPONSE MODIFYING FACTORS
SURVIVAL TIME
TOXICITY
YEARS LIVING RADIOISOTOPES