Pedersen J E, Barron G, Chapman J D
Int J Radiat Oncol Biol Phys. 1982 Mar-Apr;8(3-4):415-8. doi: 10.1016/0360-3016(82)90650-2.
Azomycin riboside (2-nitro-1-beta-D-ribofuranosylimidazole) (AR), a nucleoside analogue with the base component replaced by a 2-nitroimidazole was studied to determine its potential as a radiosensitizer. In vitro evidence showed that AR is as good as or slightly better than misonidazole (MISO) as a hypoxic cell radiosensitizer. AR was also found to kill hypoxic cells directly and this cytotoxicity was at least as great as MISO cytotoxicity. However, when tumor regrowth delay was used to assess in vivo radiosensitization, AR was found to be inferior to MISO while the LD50 host toxicity assay indicated that AR might be nearly as toxic as MISO. Unless AR proves to be less toxic than MISO or can be selectively distributed with nucleoside transport inhibitors, these preliminary observations have not shown any advantage of AR over MISO as a potential clinically useful radiosensitizer.
偶氮霉素核糖苷（2-硝基-1-β-D-呋喃核糖基咪唑）（AR）是一种核苷类似物，其碱基成分被2-硝基咪唑取代，对其作为放射增敏剂的潜力进行了研究。体外证据表明，作为低氧细胞放射增敏剂，AR与甲硝唑（MISO）效果相当或略优于MISO。还发现AR可直接杀死低氧细胞，且这种细胞毒性至少与MISO的细胞毒性一样大。然而，当用肿瘤再生长延迟来评估体内放射增敏作用时，发现AR不如MISO，而LD50宿主毒性试验表明AR的毒性可能与MISO几乎一样大。除非AR被证明毒性低于MISO，或者可以通过核苷转运抑制剂进行选择性分布，否则这些初步观察结果并未显示出AR作为一种潜在的临床有用放射增敏剂比MISO有任何优势。
