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Sc(III) Complexes of Pyclen Derivative Ligands as Probes for Hypoxia: Synthesis, Chemical Characterization, <sup>44</sup>Sc-Radiolabeling, and Preclinical Assessment.


ABSTRACT: Rigid pyclen derivative ligands bearing hypoxia-sensitive nitroimidazole (NI) pendants, PC2A-Ph-NI (hexadentate) and PC2AM-NI (heptadentate), were synthesized, radiolabeled with 44Sc(III), and evaluated under preclinical circumstances. Physicochemical characterization was carried out using the structurally related model ligand, PC2AMnBu, by multinuclear NMR, UV-Vis spectroscopy, and pH-potentiometry. Sc(III) ion was found to form a stable complex with PC2AMnBu (log KScL = 19.53(4); pSc = 19.32), in a reasonably fast reaction, with outstanding inertness (t1/2 = 529 hours in 1 M HClO4). The [Sc(PC2AMnBu)]+ complex can coordinate fluoride (log KScLF = 2.5(2)), and the ternary complex is remarkab

SUBMITTER: Csupasz T 

PROVIDER: S-EPMC12731536 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature