Conformationally Preorganized High-Affinity Ligands for Copper Biology with Hinged and Rigid Thiophene Backbones.

ABSTRACT: Copper-selective ligands are essential tools for probing the affinity of cuproproteins or manipulating the cellular copper availability. They also harbor significant potential as antiangiogenic agents in cancer therapy or as therapeutics to combat copper toxicity in Wilson's disease. To achieve the high Cu(I) affinities required for competing effectively with cellular cuproproteins, we recently devised a ligand design based on phosphine-sulfide-stabilized phosphine (PSP) donor motifs. Building on this design strategy, we integrated two PSP donors within preorganized ligand architectures composed of either a hinged bithiophene backbone (bithipPS) or a single rigid thiophene bridge (thipPS). Extensive characterization based on X-ray crystal structures, solution NMR data, spectrophotometric t

SUBMITTER: Yu J 

PROVIDER: S-EPMC10118051 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature