Edwards D I, Knox R J, Knight R C
Int J Radiat Oncol Biol Phys. 1982 Mar-Apr;8(3-4):791-3. doi: 10.1016/0360-3016(82)90736-2.
Correlations of cytotoxicity of nitroimidazoles and their electron affinity depend upon the degree of reduction of the drugs. If the end-point chosen to assess cytotoxicity is one at which incomplete reduction has occurred the slope of the correlation is positive, with respect to E71, but if measurements are taken after complete reduction of the drugs the slope is a negative one. The production of nitrite ion by 5-nitroimidazoles depends on the base composition of DNA suggesting that the active agent responsible for cytotoxicity is the one-electron radical anion, R--NO2-.
硝基咪唑类药物的细胞毒性与其电子亲和力的相关性取决于药物的还原程度。如果选择用于评估细胞毒性的终点是药物发生不完全还原的阶段,那么相关性的斜率相对于E71为正值,但如果在药物完全还原后进行测量,斜率则为负值。5-硝基咪唑类药物产生亚硝酸根离子取决于DNA的碱基组成,这表明负责细胞毒性的活性剂是单电子自由基阴离子R--NO2-。