Astor M, Hall E J, Biaglow J E, Parham J C
Int J Radiat Oncol Biol Phys. 1982 Jan;8(1):75-83. doi: 10.1016/0360-3016(82)90388-1.
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 effectiveness, 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 as consequence of its rapid removal of endogeneous cellular NPSH; which are naturally occurring radioprotective substances.
在培养的中国仓鼠细胞中,对甲硝唑与几种2、4和5取代的硝基咪唑的放射增敏效率和细胞毒性进行了比较。两种取代化合物(SR 2508和SR 2555)在放射增敏效果上与甲硝唑相似,但对缺氧细胞的毒性明显较小。这种细胞毒性的降低可能是由于药物渗透较慢或非蛋白质巯基化合物(NPSH)的清除较慢。化合物MJL-1-191-VII(一种4-硝基咪唑)是一种比根据其电子亲和力预测的更有效的放射增敏剂。它似乎通过两种机制发挥增敏作用,第一种机制是由于其电子亲和力,第二种机制是由于其快速清除内源性细胞NPSH;NPSH是天然存在的放射防护物质。