Is Smaller Better? Cu²⁺/Cu⁺ Coordination Chemistry and Copper-64 Radiochemical Investigation of a 1,4,7-Triazacyclononane-Based Sulfur-Rich Chelator.

ABSTRACT: The biologically triggered reduction of Cu²⁺ to Cu⁺ has been postulated as a possible in vivo decomplexation pathway in ^64/67Cu-based radiopharmaceuticals. In an attempt to hinder this phenomenon, we have previously developed a family of S-containing polyazamacrocycles based on 12-, 13-, or 14-membered tetraaza rings able to stabilize both oxidation states. However, despite the high thermodynamic stability of the resulting Cu^2+/+ complexes, a marked [⁶⁴Cu]Cu²⁺ release was detected in human serum, likely as a result of the partially saturated coordination sphere around the copper center. In the present work, a new hexadentate macrocyclic ligand, 1,4,7-tris[2-(methylsulfanyl)ethyl)]-1,4,7-triazacyclononane (NO3S), was s

SUBMITTER: Tosato M 

PROVIDER: S-EPMC10731632 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature