Charting the coordinative landscape of the ¹⁸F-Sc/⁴⁴Sc/¹⁷⁷Lu triad with the tri-aza-cyclononane (tacn) scaffold.

ABSTRACT: The widely established PET isotope ¹⁸F does not have a therapeutic partner. We have recently established that the Sc-F bond can be formed under aqueous, high yielding conditions, paving the way to providing ¹⁸F as diagnostic partners to ⁴⁷Sc and ¹⁷⁷Lu radiotherapeutics. Here, we synthesized a library of tacn-based chelators comprised of 10 structurally unique permutations incorporating acetate, methyl-benzylamide and picolinate donor arms. The chelator library encompasses chelators ranging from 6- to 9-dentate, and produces complex changes ranging from +3 to -1. The corresponding Sc-F/Sc and Lu chelate complexes were characterized using computational, spectroscopic and potentiometric methods, followed by optimization of radiolabeling with ¹⁸

SUBMITTER: Kelderman CAA 

PROVIDER: S-EPMC11463210 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature