Cytotoxic properties of a 4-nitroimidazole (NSC 38087): a radiosensitizer of hypoxic cells in vitro.

Abstract

5-Phenoxysulphonyl-1-methyl-4-nitroimidazole (NSC 38087) can act as a sensitizer of hypoxic mammalian cells to radiation in vitro. The degree of sensitization achieved is greater than would be predicted from the drug's electron affinity. Cytotoxicity studies have shown that 5 microM NSC 38087 can reduce the surviving fraction of log-phase V79 cells in air at 37 degrees C to 10(-2) after 2 h exposure. This toxicity is considerably increased by small rises in temperature. In contrast to other nitro-heterocyclic radiosensitizers, NSC 38087 and related 5-substituted 4-nitroimidazoles show greater toxicity towards aerobic than to hypoxic cells. Log-phase cells show the highest sensitivity to the toxic action of NSC 38087, with plateau-phase cells, cells with a history of chronic hypoxia, and thermotolerant cells showing greater resistance. These toxicity data are compared to those for the 2-nitroimidazole hypoxic-cell sensitizer misonidazole.

• Authors: I J Stratford, C Williamson, C Hardy
• Journal: British journal of cancer (Br J Cancer) Vol. 44 Issue 1 Pg. 109-16 (Jul 1981) ISSN: 0007-0920 [Print] England
• PMID: 7259957 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Nitroimidazoles
• Radiation-Sensitizing Agents
• 5-phenoxysulfonyl-1-methyl-4-nitroimidazole
• Oxygen

Topics

• Animals
• Cell Survival (drug effects, radiation effects)
• Cells, Cultured
• Cricetinae
• Cricetulus
• Dose-Response Relationship, Drug
• Nitroimidazoles (pharmacology)
• Oxygen
• Radiation-Sensitizing Agents
• Time Factors