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探讨3-硝基三氮唑衍生物的放射增敏作用,并对其生物学效应作出评价。方法本文用克隆形成法研究了22个3-硝基-1,2,4-三氮唑衍生物的体外放射增敏活性和乏氧、富氧细胞毒性。结果两个化合物的活性胜过MISO,有三个化合物与MISO和SR-2508相当,其余的其活性均较低。3-硝基三唑衍生物也像2-硝基咪唑类那样,其放射增敏活性与电子亲和性(用半波还原电位E1/2表示)有关。亲和性越大,即E1/2值越偏正,增敏活性越强。环核N1位和5位上取代基的结构和性质影响着化合物的E1/2、分配系数p和细胞毒性。结论3-硝基三唑衍生物对乏氧和富氧(空气)细胞的毒性差别是很有限的,所以它们不是有效的乏氧调节细胞毒剂。但某些的放射增敏作用是值得深入研究的。
To investigate the radiosensitization of 3-nitrotriazole derivatives and to evaluate their biological effects. Methods In this study, 22 3-nitro-1,2,4-triazole derivatives were studied in vitro for their radiosensitizing activity and hypoxia-enriched and cytotoxicity. As a result, the two compounds were more active than MISO, with three compounds comparable to MISO and SR-2508, with the remaining less active. The 3-nitrotriazole derivatives are also related to the radiosensitizing activity as the 2-nitroimidazoles and the electron affinity (represented by the half-wave reduction potential E1 / 2). The greater affinity, that is, the more positive E1 / 2 value, the stronger the sensitizing activity. The structure and properties of the substituents at the N1 and 5 positions of the cyclic nuclei affect the E1 / 2, partition coefficient p and cytotoxicity of the compounds. Conclusions 3-Nitrotriazole derivatives are very limited in their toxicity to hypoxia and oxygen-enriched (air) cells, so they are not potent hypoxia-regulating cytotoxic agents. However, some radiosensitization is worth further study.