Investigation into 64Cu-labeled Bis(selenosemicarbazone) and Bis(thiosemicarbazone) complexes as hypoxia imaging agents.

摘要: Abstract Background Cu-diacetyl-bis( N 4 -methylthiosemicarbazone) [Cu-ATSM], although excellent for oncology applications, may not be suitable delineating cardiovascular or neurological hypoxia. For this reason, new Cu hypoxia positron emission tomography (PET) imaging agents are being examined to search a higher selectivity hypoxic ischemic tissue at oxygen concentrations found in these tissues. Two approaches increase alkylation replace the sulfur atoms with selenium, resulting formation of selenosemicarbazones. Methods Three 64 Cu-labeled selenosemicarbazone complexes were synthesized and one was screened vitro using EMT-6 mouse mammary carcinoma cells. Rodent biodistribution small animal PET images obtained from BALB/c mice implanted tumors. One alkylated thiosemicarbazone examined. Results Of three bis(selenosemicarbazone) ligands examined, only Cu-diacetyl-bis(selenosemicarbazone) [ Cu-ASSM] isolated high-enough radiochemical purity undertake cell uptake experiments where shown independent concentration. The bis(thiosemicarbazone) complex synthesized, -ethylthiosemicarbazone) Cu-ATSE], showed similar Cu-ATSM Biodistribution studies Cu-ASSM Cu-ATSE high tumor 20 min ( Cu-ASSM, 10.33±0.78% ID/g; Cu-ATSE, 7.71±0.46% ID/g). tumor-bearing visualized revealed consistent data. Conclusion compounds could vivo. Although stability increased upon addition methyl groups diimine backbone, fully species, demonstrated no selectivity. However, additional present modifies vivo properties when compared Cu-ATSM.