Potential radiosensitizing agents. 5. 2-Substituted benzimidazole derivatives
| Autor: | Rajender P. Gupta, Cynthia A. Larroquette, Krishna C. Agrawal |
|---|---|
| Rok vydání: | 1982 |
| Předmět: |
Radiation-Sensitizing Agents
Benzimidazole Chemical Phenomena Cell Survival Epoxide Chinese hamster Potassium carbonate chemistry.chemical_compound Cricetulus Cricetinae Drug Discovery Animals Organic chemistry Cells Cultured Oxazole biology Chemistry Physical biology.organism_classification Combinatorial chemistry chemistry Gamma Rays Cell culture Yield (chemistry) Molecular Medicine Benzimidazoles Radiosensitizing Agent |
| Zdroj: | Journal of Medicinal Chemistry. 25:1342-1346 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00353a014 |
| Popis: | A series of 2-substituted benzimidazoles and their derivatives have been synthesized and tested for their ability to selectively sensitize hypoxic Chinese hamster cells (V-79) toward the lethal effect of ionizing radiation. These compounds were prepared by reacting the 2-substituted benzimidazoles with 1,2-epoxy-3-methoxypropane in the presence of potassium carbonate. Reaction of the 2-nitro and 2-methylfonyl analogue with the epoxide also yielded a cyclized material, which was confirmed to be a benzimidazo[2,1-b]oxazole. In an attempt to increase the electron affinity, 5- or 6-nitro-2-substituted-benzimidazoles were also synthesized and then reacted with the epoxide to yield the corresponding 1-substituted derivatives. The results of the biological tests for the radiosensitizing activity of these agents against Chinese hamster cells (V-79) in culture indicated that the 2-nitro-substituted analogues were the most effective sensitizers in this series. |
| Databáze: | OpenAIRE |
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