Edwards D I, Knox R J, Skolimowski I M, Zahoor A, Knight R C
Int J Radiat Oncol Biol Phys. 1984 Aug;10(8):1319-22. doi: 10.1016/0360-3016(84)90340-7.
RSU 1069 is a 2-nitroimidazole radiosensitizer with an aziridine-containing side chain. In light (360 nm) the absorbance maximum of the nitro group at 325 nm disappears, which is accompanied by expulsion of the nitro group as the nitrite ion. We suggest an intramolecular cyclization of the aziridine side chain and the C2 of the imidazole ring as a possible explanation. This photosensitive effect was used to determine separately the damage to DNA induced by the reduced nitro group and the alkylating property of the aziridine. The aziridine-induced DNA damage is maximized in the dark when the nitro group is either absent (electrolytically reduced prior to the addition of DNA) or non functional (unreduced). In the light, damage is reduced. Typical DNA damage includes helix disruption leading to single strand breaks and the release of thymidine. Alkaline filter elution studies show evidence only for strand breakage and none for cross-linking indicating the drug is capable of mono-functional alkylation only.
RSU 1069是一种带有含氮丙啶侧链的2-硝基咪唑类放射增敏剂。在光照（360纳米）下，硝基在325纳米处的最大吸收峰消失，同时伴随着硝基以亚硝酸根离子的形式被逐出。我们提出氮丙啶侧链与咪唑环的C2发生分子内环化是一种可能的解释。这种光敏效应被用于分别测定还原硝基诱导的DNA损伤以及氮丙啶的烷基化特性。当硝基不存在（在加入DNA之前进行电解还原）或无功能（未还原）时，氮丙啶诱导的DNA损伤在黑暗中达到最大值。在光照下，损伤会减少。典型的DNA损伤包括导致单链断裂的螺旋破坏以及胸腺嘧啶的释放。碱性滤膜洗脱研究仅显示出链断裂的证据，没有交联的证据，表明该药物仅能进行单功能烷基化。
