Rigid H4OCTAPA derivatives as model chelators for the development of Bi(III)-based radiopharmaceuticals

Fátima Lucio-Martínez; David Esteban-Gómez; Laura Valencia; Dávid Horváth; Dániel Szücs; Anikó Fekete; Dezső Szikra; Gyula Tircsó; Carlos Platas-Iglesias

doi:10.1039/d2cc06876a

Rigid H₄OCTAPA derivatives as model chelators for the development of Bi(III)-based radiopharmaceuticals

Chem Commun (Camb). 2023 Mar 16;59(23):3443-3446. doi: 10.1039/d2cc06876a.

Authors

Affiliations

¹ Universidade 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.
² Departamento de Química Inorgánica, Facultad de Ciencias, Universidade de Vigo, As Lagoas, Marcosende, Pontevedra 36310, Spain.
³ Department of Physical Chemistry, Faculty of Science and Technology, University of Debrecen, Egyetem tér 1, Debrecen H-4032, Hungary. gyula.tircso@science.unideb.hu.
⁴ Doctoral School of Chemistry, Faculty of Science and Technology, University of Debrecen, Egyetem tér 1, Debrecen H-4032, Hungary.
⁵ Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei krt. 98., Debrecen H-4032, Hungary. fekete.aniko@science.unideb.hu.

PMID: 36857648
DOI: 10.1039/d2cc06876a

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.

MeSH terms

Bismuth / chemistry
Chelating Agents*
Ligands
Radiopharmaceuticals*

Substances

Chelating Agents
Ligands
Radiopharmaceuticals
Bismuth