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Iodoglucoazomycin (I‐GAZ;  N ‐(2‐iodo‐3‐(6‐ O ‐glucosyl)propyl)‐2‐nitroimidazole), a non‐glycosidic nitroimidazole–6‐ O ‐glucose adduct, was synthesized, radioiodinated, and evaluated as a substrate of glucose transporter 1 (GLUT1) for radiotheranostic (therapy+diagnostic) management of hypoxic tumors. Nucleophilic iodination of the nosylate synthon of I‐GAZ followed by deprotection afforded I‐GAZ in 74 % overall yield. I‐GAZ was radioiodinated via ‘exchange’ labeling using [ 123/131 I]iodide (50–70 % RCY) and then purified by Sep‐Pak™ (>96 % RCP). [ 131 I]I‐GAZ was stable in 2 % ethanolic solution in sterile water for 14 days when stored at 5 °C. In cell culture, I‐GAZ was found to be nontoxic to EMT‐6 cells at concentrations <0.5 m m , and weakly radiosensitizing (SER 1.1 at 10 % survival of EMT‐6 cells; 1.2 at 0.1 % survival in MCF‐7 cells). The hypoxic/normoxic uptake ratio of [ 123 I]I‐GAZ in EMT‐6 cells was 1.46 at 2 h, and under normoxic conditions the uptake of [ 123 I]I‐GAZ by EMT‐6 cells was unaltered in the presence of 5 m m  glucose. The biodistribution of [ 131 I]I‐GAZ in EMT‐6 tumor‐bearing Balb/c mice demonstrated rapid clearance from blood and extensive renal and hepatic excretion. Tumor/blood and tumor/muscle ratios reached ∼3 and 8, respectively, at 4 h post‐injection. Regression analysis of the first order polynomial plots of the blood and tumor radioactivity concentrations supported a perfusion–excretion model with low hypoxia‐dependent binding. [ 131 I]I‐GAZ was found to be stable in vivo, and did not deiodinate.

chemmedchem

Synthesis and Biological Evaluation of Iodoglucoazomycin (I‐GAZ), an Azomycin–Glucose Adduct with Putative Applications in Diagnostic Imaging and Radiotherapy of Hypoxic Tumors