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†

Fátima Lucio-Martínez,

^a David Esteban-Gómez,

^a Laura Valencia,

^b Dávid Horváth,^cd Dániel Szücs,^cde Anikó Fekete,*^e Dezső Szikra,^e Gyula Tircsó

*^c and Carlos Platas-Iglesias

*^a

Author affiliations

* Corresponding authors

^a Universidade da Coruña, Centro de Investigacións Científicas Avanzadas (CICA) and Departamento de Química, Facultade de Ciencias, A Coruña, Galicia, Spain
E-mail: carlos.platas.iglesias@udc.es

^b Departamento de Química Inorgánica, Facultad de Ciencias, Universidade de Vigo, As Lagoas, Marcosende, Pontevedra 36310, Spain

^c Department of Physical Chemistry, Faculty of Science and Technology, University of Debrecen, Egyetem tér 1, Debrecen H-4032, Hungary
E-mail: gyula.tircso@science.unideb.hu

^d Doctoral School of Chemistry, Faculty of Science and Technology, University of Debrecen, Egyetem tér 1, Debrecen H-4032, Hungary

^e Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei krt. 98., Debrecen H-4032, Hungary
E-mail: fekete.aniko@science.unideb.hu

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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DOI: https://doi.org/10.1039/D2CC06876A
Article type: Communication
Submitted: 17 Dec 2022
Accepted: 21 Feb 2023
First published: 21 Feb 2023

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Chem. Commun., 2023,59, 3443-3446

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

F. Lucio-Martínez, D. Esteban-Gómez, L. Valencia, D. Horváth, D. Szücs, A. Fekete, D. Szikra, G. Tircsó and C. Platas-Iglesias, Chem. Commun., 2023, 59, 3443 DOI: 10.1039/D2CC06876A

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Chemical Communications

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

Abstract

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

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