Inorganic Chemistry· 2026Q1
Picolinate- and Phosphonated Pyridyl-TACN Ligands for Highly Stable and Inert Cu(II) Complexes for Radiochemical Applications
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- Q1SCImago
- 2026year
Short summary
Two novel phosphonated pyridine-TACN ligands form highly stable 64Cu complexes suitable for renal-excreted PET imaging, outperforming a lipophilic picolinate analogue.
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Key points
- Three novel TACN-based chelators with picolinate and phosphonated pyridine arms were synthesized.
- These ligands form stable Cu(II) complexes with an optimal five-coordinate geometry.
- 64Cu complexes of phosphonated pyridine-TACN ligands showed renal excretion in PET imaging.
- A picolinate-TACN analogue exhibited lipophilicity and partial liver excretion.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract In this study, three novel chelators based on the 1,4,7-triazacyclononane (TACN) ligand platform were introduced. The ligands contain picolinate and phosphonated pyridine chelating arms to provide an optimal five-coordinate geometry for Cu(II). The solution chemistry of these complexes was systematically investigated using spectrophotometric titrations, UV-vis spectroscopy, electron paramagnetic resonance (EPR), and cyclic voltammetry (CV). Then, these ligands were employed in 64Cu radiolabeling studies and subsequent in vivo positron emission tomography (PET) imaging studies to reveal that the 64Cu complexes of the two phosphonated pyridine-TACN ligands were excreted via the renal pathway, while the picolinate-TACN analogue exhibited a shift in the excretion pathway due to its lipophilic nature, resulting in partial liver excretion. To our knowledge, the use of phosphonated pyridines as chelators in 64Cu PET imaging is uncommon, which underscores the significance of this study.
The authors' abstract, as published at the source. Inorganic Chemistry, 2026 · DOI ↗
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Field: Radiology, Nuclear Medicine and Imaging
Radiology, Nuclear Medicine and ImagingMedicine