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Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Rigid H4OCTAPA derivatives as model chelators for the development of Bi(III)-based radiopharmaceuticals
Fátima Lucio-Martínez1, David Esteban-Gómez1, Laura Valencia2
1Universidade da Coruña, Centro de Investigacións Científicas Avanzadas (CICA) and Departamento de Química, Facultade de Ciencias, 15071, A Coruña, Galicia, Spain. carlos.platas.iglesias@udc.es.
Abstract:
Octadentate ligands containing ethyl (H4OCTAPA), cyclohexyl (H4CHXOCTAPA) or cyclopentyl (H4CpOCTAPA) spacers were assessed as chelators for Bi(III)-based radiopharmaceuticals. The H4CHXOCTAPA chelator displays excellent properties, including 205/206Bi-nuclide radiolabelling under mild conditions, excellent stability in serum and in the presence of competing cations or H5DTPA. The poor performance of H4CpOCTAPA appears to be related to the stereochemical activity of the Bi(III) lone pair.
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