Newly synthesized hypoxia-mediated drugs as radiosensitizers and cytotoxic agents

Journal Article · Fri Jan 01 04:00:00 EST 1982 · Int. J. Radiat. Oncol., Biol. Phys.; (United States)

DOI:https://doi.org/10.1016/0360-3016(82)90388-1· OSTI ID:6712619

Astor, M ^[1]; Hall, E J; Bigalow, J E; Parham, J C

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1. Columbia Univ., New York, NY

Chinese hamster cells in culture were used to compare the radiosensitizing efficiency and cytotoxicity of misonidazole with several 2, 4 and 5 substituted nitroimidazoles. The two substituted compounds (SR 2508 and SR 2555) are similar to misonidazole in radiosensitizing effectivenss, but are significantly less toxic to hypoxic cells. This reduced cytotoxicity may result from either slower drug penetration or slower removal of non-protein sulfhydryl compounds (NPSH). The compound MJL-1-191-VII* (a 4-nitroimidazole) is a much more effective radiosensitizer than would be predicted from its electron affinity. It appears to sensitize by two mechanisms, the first resulting from its electron affinity and the second a consequence of its rapid removal of endogeneous cellular NPSH; which are naturally occurring radioprotective substances.

• OSTI ID: 6712619
• Journal Information: Int. J. Radiat. Oncol., Biol. Phys.; (United States), Journal Name: Int. J. Radiat. Oncol., Biol. Phys.; (United States) Vol. 8:1; ISSN IOBPD
• Country of Publication: United States
• Language: English

Related Subjects

560121 -- Radiation Effects on Cells-- External Source-- (-1987)
560301* -- Chemicals Metabolism & Toxicology-- Cells-- (-1987)
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AFFINITY
ANIMAL CELLS
ANIMALS
ANOXIA
ANTINEOPLASTIC DRUGS
AZOLES
CELL CULTURES
COMPARATIVE EVALUATIONS
CONNECTIVE TISSUE CELLS
DRUGS
ELEMENTS
FIBROBLASTS
HAMSTERS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
MAMMALS
MISONIDAZOLE
NITRO COMPOUNDS
NONMETALS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
OXYGEN
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
RODENTS
SOMATIC CELLS
THIOLS
TOXICITY
VERTEBRATES