Tuning the Kinetic Inertness of Bi³⁺ Complexes: The Impact of Donor Atoms on Diaza-18-Crown-6 Ligands as Chelators for ²¹³Bi Targeted Alpha Therapy.

ABSTRACT: The radionuclide ²¹³Bi can be applied for targeted α therapy (TAT): a type of nuclear medicine that harnesses α particles to eradicate cancer cells. To use this radionuclide for this application, a bifunctional chelator (BFC) is needed to attach it to a biological targeting vector that can deliver it selectively to cancer cells. Here, we investigated six macrocyclic ligands as potential BFCs, fully characterizing the Bi³⁺ complexes by NMR spectroscopy, mass spectrometry, and elemental analysis. Solid-state structures of three complexes revealed distorted coordination geometries about the Bi³⁺ center arising from the stereochemically active 6s² lone pair. The kinetic properties of the Bi³⁺ complexes were assessed by challenging them wit

SUBMITTER: Fiszbein DJ 

PROVIDER: S-EPMC8491275 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature