Roberts P B, Denny W A, Cain B F
Br J Cancer. 1979 Oct;40(4):641-8. doi: 10.1038/bjc.1979.230.
Six anilinoacridine derivatives have been tested for the ability to act as radiosensitizers. Two gave good sensitization at concentrations of 100 microM or less. Both of these are known to possess significant activity against experimental tumours, and one (m-AMSA) is in Phase II clinical trial as a chemotherapeutic drug. Anilinoacridines may have potential as drugs with both a chemotherapeutic and radiosensitizing role. In spite of their structural similarity, the 2 derivatives which sensitize do so by different mechanisms. Compound VI behaves like a typical hypoxic cell sensitizer but Compound I (m-AMSA) interferes with the accumulation of sublethal damage in either the presence or absence of O2. The latter also displays a post-irradiation sensitizing effect. Differences in mechanism may be related to the relative DNA-binding abilities and electronic differences between the 2 drugs.
已对六种苯胺吖啶衍生物作为放射增敏剂的作用能力进行了测试。其中两种在浓度为100微摩尔或更低时表现出良好的增敏作用。已知这两种衍生物对实验性肿瘤均具有显著活性，其中一种（m-AMSA）作为化疗药物正处于II期临床试验阶段。苯胺吖啶类药物可能具有作为兼具化疗和放射增敏作用的药物的潜力。尽管它们结构相似，但两种具有增敏作用的衍生物的作用机制不同。化合物VI表现得像典型的乏氧细胞增敏剂，而化合物I（m-AMSA）在有氧或无氧条件下均会干扰亚致死损伤的积累。后者还表现出辐照后增敏效应。作用机制的差异可能与这两种药物相对的DNA结合能力和电子差异有关。
