Watts M E, Jacobs R S
Br J Cancer Suppl. 1978 Jun;3:80-3.
Studies using V79 379A cells on about 50 nitroaromatic and nitroheterocyclic radisosensitizers have confirmed the relationship between sensitizing efficiency and electron affinity. Almost all the compounds studied behaved similarly by sensitizing hypoxic cells to X-irradiation in a dose-modifying manner whilst having no sensitizing effect on oxygenated cells. However, a small number of the radiosensitizers studied exhibited additional or atypical properties. A 4-nitroimidazole ring substituted with chlorine sensitized hypoxic cells much more efficiently than predicted from its redox potential. A 2-nitroimidazole substituted with a carboxylic acid side chain showed a low but constant level of sensitization over 5 decades of concentration. A 5-nitrofuran, in addition to sensitizing hypoxic cells by dose modification, sensitized oxygenated cells by a reduction in extrapolation number.
使用V79 379A细胞对约50种硝基芳香族和硝基杂环辐射增敏剂进行的研究证实了增敏效率与电子亲和力之间的关系。几乎所有研究的化合物表现相似,即以剂量修饰的方式使缺氧细胞对X射线辐射敏感,而对含氧细胞无增敏作用。然而,少数研究的辐射增敏剂表现出额外的或非典型的特性。一个被氯取代的4-硝基咪唑环比根据其氧化还原电位预测的更有效地使缺氧细胞敏感。一个被羧酸侧链取代的2-硝基咪唑在5个数量级的浓度范围内显示出低但恒定的增敏水平。一种5-硝基呋喃,除了通过剂量修饰使缺氧细胞敏感外,还通过降低外推数使含氧细胞敏感。