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Evaluation of 2-amino-5-nitrothiazole as a hypoxic cell radiosensitizer

Journal Article · · Radiat. Res.; (United States)
DOI:https://doi.org/10.2307/3575735· OSTI ID:7085374
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The nitroheterocyclic compound 2-amino-5-nitrothiazole (ANT) was evaluated as a hypoxic radiosensitizer. Experiments with bacteria showed that this agent was similar to misonidozole in radiosensitizing activity, but was less cytotoxic and less mutagenic than misonidazole. Experiments with EMT6 tumor cells in culture showed ANT to be an effective hypoxic radiosensitizer, although slightly less active than misonidazole, and to be less cytotoxic than misonidazole. ANT was more toxic to mice than misonidazole and produced a spectrum of symptoms, including hyperactivity and agitation, different from those of misonidazole. The toxicities of ANT and misonidazole were additive. The maximum levels of ANT achieveable in the tumors after ip injection of nontoxic doses of drug were low (<3 x 10/sup -4/ M) and the radiosensitization obtainable with the drug in vivo was inferior to that obtainable with misonidazole. These findings suggest that nitrothiazoles might be an interesting class of nitroheterocyclic radiosensitizers, but that molecules with increased solubility and improved pharmacokinetics would be necessary for efficacy in vivo.

Research Organization:
Yale Univ. School of Medicine, New Haven, CT
OSTI ID:
7085374
Journal Information:
Radiat. Res.; (United States), Journal Name: Radiat. Res.; (United States) Vol. 90:3; ISSN RAREA
Country of Publication:
United States
Language:
English

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Related Subjects

560120 -- Radiation Effects on Biochemicals
Cells
&amp; Tissue Culture
560152* -- Radiation Effects on Animals-- Animals
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMAL CELLS
ANIMALS
AZOLES
BACTERIA
BIOLOGICAL EFFECTS
CELL KILLING
DRUGS
ELECTROMAGNETIC RADIATION
ESCHERICHIA COLI
EVALUATION
HETEROCYCLIC COMPOUNDS
INJECTION
INTAKE
INTRAPERITONEAL INJECTION
IONIZING RADIATIONS
MAMMALS
MICE
MICROORGANISMS
NITRO COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
RADIATIONS
RADIOSENSITIVITY
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
RODENTS
THIAZOLES
TUMOR CELLS
VERTEBRATES
X RADIATION