Microwave gallium-68 radiochemistry for kinetically stable bis(thiosemicarbazone) complexes: structural investigations and cellular uptake under hypoxia
作者： Israt S. Alam , Rory L. Arrowsmith , Fernando Cortezon-Tamarit , Frazer Twyman , Gabriele Kociok-Köhn
DOI: 10.1039/C5DT02537K
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摘要: We report the microwave synthesis of several bis(thiosemicarbazones) and rapid gallium-68 incorporation to give corresponding metal complexes. These proved kinetically stable under ‘cold’ ‘hot’ biological assays were investigated using laser scanning confocal microscopy, flow cytometry radioactive cell retention studies normoxia hypoxia. 68Ga complex was found be 34% higher in hypoxic cells than normoxic over 30 min, further increasing 53% at 120 min. Our data suggests that this class gallium complexes show hypoxia selectivity suitable for imaging living vivo tests by microPET nude athymic mice showed they are excreted within 1 h their administration.
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