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Date publication
mai 2026
Journal
Inorganic chemistry
Auteurs
Membres identifiés du Cancéropôle Est :
Dr ELHABIRI Mourad
Tous les auteurs :
Petitpoisson L, Demartinecourt T, Elhabiri M, Le Guennic B, Huclier-Markai S, Nonat AM
Lien Pubmed
Résumé
Scandium radioisotopes (Sc, Sc, and Sc) show strong promise for PET imaging and targeted radiotherapy. Their use requires the development of bifunctional chelators (BFCs) that can complex these metallic isotopes under mild conditions while maintaining a high stability. This study reports the synthesis and evaluation of two novel bispidine-based ligands for Sc(III) complexation, with a particular focus on , which incorporates two picolinate substituents. The radiolabeling behavior, as well as the thermodynamic and kinetic properties of the corresponding Sc(III) complexes, were investigated. Ligand readily formed a stable 1:1 Sc(III) complex at room temperature, adopting a . Thermodynamic studies confirmed high stability (log = 14.84, pSc = 10.7) and a notable preference for Sc(III) over Tb(III) (pTb = 7.8). enabled quantitative radiolabeling of Sc at room temperature within 15 min (pH 6, M:L = 1:20). The complex is stable in human serum with no detectable decomplexation over 4 h and showed only partial decomplexation in hydroxyapatite challenge experiments. Successful radiolabeling with Sc further highlighted its versatility. Together, these findings highlight the significant potential of the bispidine-based ligands. In particular, emerges as a promising platform for future developments in Sc-based radiopharmaceuticals and theragnostics.
Référence
Inorg Chem. 2026 05 20;:
