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

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. Key words: N- (5-nitroindazole-3-formyl) tyrosine sodium; Neoplasms; hypoxic radiosensitization; biodistribution