Evaluating a triaza-18-crown-6 picolinate chelator for [212/203Pb]Pb2+ and [212/213Bi]Bi3+ theranostics

Desiree Fiaccabrino; Tinotenda Masvikeni; Brooke L. McNeil; Brian O. Patrick; María de Guadalupe Jaraquemada-Peláez; Paul Schaffer; Chris Orvig

doi:10.1039/D5DT01103E

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Evaluating a triaza-18-crown-6 picolinate chelator for [^212/203Pb]Pb²⁺ and [^212/213Bi]Bi³⁺ theranostics†

Desiree Fiaccabrino,^ab Tinotenda Masvikeni,^a Brooke L. McNeil,^bc Brian O. Patrick,^d María de Guadalupe Jaraquemada-Peláez,*^e Paul Schaffer

*^bcf and Chris Orvig

*^a

Author affiliations

* Corresponding authors

^a Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada
E-mail: orvig@chem.ubc.ca

^b Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, Vancouver, British Columbia, Canada

^c Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, Canada

^d Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada

^e Department of Molecular Oncology, BC Cancer Research Institute, Vancouver, Canada

^f Department of Radiology, University of British Columbia, Vancouver, British Columbia V5Z 1M9, Canada

Abstract

H₃tripa (H₃macrotripa), a triaza-18-crown-6 macrocycle bearing three picolinate arms, enables quantitative radiolabeling of [²⁰³Pb]Pb²⁺ and [²¹³Bi]Bi³⁺ and exhibits robust human serum stability. NMR spectroscopy, X-ray crystallography, density functional theory, and UV-potentiometry investigate its coordination geometry and thermodynamics with Bi³⁺ and Pb²⁺, highlighting H₃tripa as a promising Pb/Bi theranostic chelator.

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Article information

DOI: https://doi.org/10.1039/D5DT01103E
Article type: Communication
Submitted: 09 May 2025
Accepted: 26 Jun 2025
First published: 14 Jul 2025

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Dalton Trans., 2025,54, 11801-11807

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Evaluating a triaza-18-crown-6 picolinate chelator for [^212/203Pb]Pb²⁺ and [^212/213Bi]Bi³⁺ theranostics

D. Fiaccabrino, T. Masvikeni, B. L. McNeil, B. O. Patrick, M. D. G. Jaraquemada-Peláez, P. Schaffer and C. Orvig, Dalton Trans., 2025, 54, 11801 DOI: 10.1039/D5DT01103E

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