Targeted Tumor Radiotherapy Sensitizer-nies Compounds

Research on targeting radiosensitizers——nitroinzadole derivatesIn order to search for the new safe and effective radiosensitizers with high potency,Using 5-nitroindazole-3-carboxylic acid as a lead compound, and based on the principles of hybridization with amino acid,a series of 5-nitroindazole derivates were designed and synthesized.The products were synthesized by direct condensation of 5-nitroindazole-3-carboxylic acid and amino acid esters.We named the six products as NIES.To investigate their cytotoxicity and radiosensitization,we performed two experiments,one was cell test in Hela and the other was animal test in kunming mice,both of the two tests showed positive result in radiosensitization,and lower cytotoxixity to cells and mice.To investigate the six compounds wether have targeting action to tumor tissues or not we studyied the in vivo distribution of 5-Nitroindazole-3-formyl tyrosine which is radiolabelled by ¹²⁵I,and the results showed this compound have a high ratio of tumor to background.Altogether,this study showed that the transformation of 5-nitroindazole by this means is feasible.