Abstract
Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.
Highlights
Chemical methods for the assembly of metal complexes are based on coordinate bonds and weak interactions
We demonstrated that 4N-coordinated platinum complexes exhibited 20S proteasome-inhibitory activities [32]
The chemical structures of platinum complexes are shown in scheme 1
Summary
Chemical methods for the assembly of metal complexes are based on coordinate bonds and weak interactions. Weak interactions such as electrostatic bonding, hydrogen bonding and aromatic ring stacking play vital roles in molecular recognition in vivo. Non-covalent interactions involving aromatic rings (e.g. aromatic–aromatic interactions and hydrophobic interactions) have many characteristics and are very interesting.
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