N-（5-硝基吲唑-3-甲酰）酪氨酸钠的制备、乏氧增敏与体内分布研究

Synthesis, hypoxic radiosensitization and biodistribution of N-(5-nitroindazole-3-formyl)tyrosine sodium

    摘要
  • 摘要:
    目的 在硝基吲唑母核上引入酪氨酸并成盐，制备N-（5-硝基吲唑-3-甲酰）酪氨酸钠并考察其乏氧增敏活性和体内分布情况。
    方法 用缩合剂法合成N-（5-硝基吲唑-3-甲酰）酪氨酸钠，通过小鼠移植瘤模型评价其乏氧增敏活性，通过放射性碘标记法考察其在荷瘤小鼠体内的分布情况。
    结果 合成了目标化合物并对结构进行了确证。移植瘤模型增敏实验表明其对H22移植瘤具有一定的乏氧增敏活性，平均放射增敏比为1.5。体内分布实验中其在肿瘤部位与脑和肌肉部位的分布比值均大于5，表明其具有较好的体内分布特性。
    结论 N-（5-硝基吲唑-3-甲酰）酪氨酸钠具有良好的乏氧增敏活性和体内分布特性，具有进一步开发价值。

     

    Abstract:
    Objective To synthesize N-(5-nitroindazole-3-formyl)tyrosine sodium and investigate its hypoxic radiosensitizing effect and biodistribution.
    Method Synthesized the target compound(N-(5-nitroindazole-3-formyl)tyrosine sodium)using condensing agents, and investigated its radiosensitization under hypoxia using H22 xenograft models and its biodistribution using radioactive iodine labeling.
    Results The synthesis and structure of the target compound were confirmed. Xenograft models showed that it had a certain radiosensitizing activity and the mean value of sensitization enhancement ratio was 1.5. Biodistribution experiment revealed that it had a good distribution manner, the distribution ratios of tumor to the nervous system and muscle were both greater than 5.
    Conclusion N-(5-nitroindazole-3-formyl)tyrosine sodium had good radiosensitizing activity and biodistribution manner, and it was worthy of further study.

     

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