Multifunctional Desferrichrome Analogues as Versatile ⁸⁹Zr(IV) Chelators for ImmunoPET Probe Development.

ABSTRACT: New bifunctional hexa- and octadentate analogues of the hydroxamate-containing siderophore desferrichrome (DFC) have been synthesized and evaluated as ⁸⁹Zr-chelating agents for immunoPET applications. The in vitro and in vivo inertness of these new ligands, Orn3-hx (hexadentate) and Orn-4hx derivatives (octadentate), was compared to the gold standard hexadentate, hydroxamate-containing chelator for ⁸⁹Zr desferrioxamine (DFO). Density functional theory was employed to model the geometries of the resulting Zr(IV) complexes and to predict their relative stabilities as follows: Zr(Orn4-hx) > Zr(DFC) > Zr(Orn3-hx). Transchelation challenge experiments of the corresponding radiochemical complexes with excess ethylenediaminetetraacetate (EDTA) indicated complex stability in

SUBMITTER: Adams CJ 

PROVIDER: S-EPMC5600883 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature