@article{Siakalli:2026:10.1039/d5dt03015c,
author = {Siakalli, C and Osborne, BE and Brown, RK and Rocco, C and Weiss, D and García-España, EV and Grundler, PV and Moiseeva, AN and Talip, Z and van, der Meulen NP and Ma, MT and Long, NJ},
doi = {10.1039/d5dt03015c},
journal = {Dalton Trans},
title = {Hydroxyquinoline-functionalised aza-crown macrocycles for lanthanide coordination.},
url = {http://dx.doi.org/10.1039/d5dt03015c},
year = {2026}
}

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TY  - JOUR
AB  - Emerging therapeutic radiolanthanides have utility for systemic molecular radiotherapy in nuclear medicine, provided that suitable chemical technology is available to incorporate them into receptor-targeted radiopharmaceuticals. In this work, N,N'-bis(8-hydroxyquinoline-2-ylmethyl)-4,13-diaza-18-crown-6 (H2KHQ) was synthesised, and its binding ability, thermodynamic stability and selectivity for Ln3+ ions (Ln3+ = La, Tb, and Lu) investigated. The design of H2KHQ involves pendant arms featuring 8-hydroxyquinoline units, known to possess metal-chelating properties and desirable activity in other therapeutic molecules. H2KHQ exhibited selectivity for the larger Ln3+ ions, confirmed by experimentally measured stability constants as well as DFT calculations. H2KHQ was able to bind the larger, non-radioactive La3+ and Tb3+ ions within 30 minutes at room temperature, forming a single, 2-fold symmetric species in solution. The structure of [La-HKHQ]2+, as determined by single crystal XRD, emphasized the need for high denticity chelators to satisfy the coordination sphere of the Ln3+, showing a 10-coordinate La3+ metal centre. H2KHQ was radiolabelled with [161Tb]TbCl3 under mild conditions in 92% radiochemical yield in promising proof-of-concept measurements.
AU  - Siakalli,C
AU  - Osborne,BE
AU  - Brown,RK
AU  - Rocco,C
AU  - Weiss,D
AU  - García-España,EV
AU  - Grundler,PV
AU  - Moiseeva,AN
AU  - Talip,Z
AU  - van,der Meulen NP
AU  - Ma,MT
AU  - Long,NJ
DO  - 10.1039/d5dt03015c
PY  - 2026///
TI  - Hydroxyquinoline-functionalised aza-crown macrocycles for lanthanide coordination.
T2  - Dalton Trans
UR  - http://dx.doi.org/10.1039/d5dt03015c
UR  - https://www.ncbi.nlm.nih.gov/pubmed/41636114
ER  - 

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