Rupp W D, Mroczkowski Z, Agrawal K C
Br J Cancer Suppl. 1978 Jun;3:60-3.
Several radiosensitizing chemicals, including a family of simple nitroimidazoles, were examined in E. coli and compared with misonidazole for toxic side-effects on endpoints such as mutagenesis, cell killing and inhibition of the synthesis of the inducible enzyme beta-galactosidase. While all the compounds were similar to misonidazole or better in radiosensitization, marked differences in the various side effects were found. There results show that for E. coli it is possible to find compounds that sensitize as well as misonidazole but which have decreased mutagenicity and fewer other side-effects. Of the compounds examined, KA121 (2,5-dinitroimidazole) is the most promising for future study because it combines good radiosensitization with low mutagenicity and toxicity.
研究人员在大肠杆菌中检测了几种放射增敏化学物质，包括一类简单的硝基咪唑，并将其与米索硝唑进行比较，以研究它们对诸如诱变、细胞杀伤和诱导型β-半乳糖苷酶合成抑制等终点的毒性副作用。虽然所有化合物在放射增敏方面与米索硝唑相似或更优，但发现它们在各种副作用方面存在显著差异。这些结果表明，对于大肠杆菌而言，有可能找到与米索硝唑一样具有增敏作用但诱变活性降低且其他副作用较少的化合物。在所检测的化合物中，KA121（2,5-二硝基咪唑）最有希望用于未来的研究，因为它兼具良好的放射增敏作用以及低诱变活性和毒性。
