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[摘要]：The copper(II) bisthiosemicarbazonato complex, copper-diacetyl-bis(N4-methylthiosemicarbazonate) (Cu-ATSM), has been used clin. as a positron emission tomog. (PET) tracer for the derived from diacetyl-2-(4-N-methyl-3-thiosemicarbazone)-3-(4-N-amino-3-thiosemic arbazone) (H2ATSM/A), one of which contained a nitroimidazole functionality, were radiolabeled with 64Cu (t1/2 = 12.7 h, b+ = 19.3%). In vitro studies were performed on three of the compds. using EMT6 mammary carcinoma cells under hypoxic and normoxic conditions. All compds. displayed rapid cellular assocn. and appreciable hypoxic selectivity with increased uptake under normoxic and hypoxic conditions when compared to 64Cu-ATSM. Biodistribution and small animal PET imaging studies were then carried out in vivo using two compds. in EMT6 tumor-bearing mice. The compds. showed high tumor uptake, but also substantial accumulation in the liver. These complexes demonstrate that H2ATSM/A represents a novel and versatile synthetic platform that can be utilized to provide hypoxic cell selectivity through functionalization of the bisthiosemicarbazonate group. |
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