Structural Variations and Formation Constants of First-Row Transition Metal Complexes of Biologically Active Aroylhydrazones

  title={Structural Variations and Formation Constants of First-Row Transition Metal Complexes of Biologically Active Aroylhydrazones},
  author={Claire M. Armstrong and Paul V. Bernhardt and Piao Chin and Des R. Richardson},
  journal={European Journal of Inorganic Chemistry},
Iron chelators of the 2-pyridinecarbaldehyde isonicotinoylhydrazone (HPCIH) class show high potential for the treatment of iron overload diseases. In the present study, selected first-row transition metal (from Mn to Zn) complexes with HPCIH and 2-pyridinecarbaldehyde (4'-aminobenzoyl)hydrazone (HPCAH) were synthesised and characterised. Crystallography reveals that HPCAH exclusively forms bis complexes with divalent transition metals, with each ligand coordinating meridionally through its… 

Cytotoxic iron chelators: characterization of the structure, solution chemistry and redox activity of ligands and iron complexes of the di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) analogues

Collectively, studies on the solution chemistry and structure of these HPKIH analogues indicate that they can bind cellular Fe and enhance its redox activity, resulting in oxidative damage to vital biomolecules.

Hydrazone chelators for the treatment of iron overload disorders: iron coordination chemistry and biological activity.

An extensive study of the Fe coordination chemistry of the HPCIH analogues including the first crystallographically characterised Fe(II) complex of these chelators, which indicates that their Fe chelation efficacy is due, at least in part, to the fact that these ligands and their Fe( II) complexes are neutral at physiological pH (7.4) and sufficiently lipophilic to permeate cell membranes.

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Tuning the antiproliferative activity of biologically active iron chelators: characterization of the coordination chemistry and biological efficacy of 2-acetylpyridine and 2-benzoylpyridine hydrazone ligands

Novel structure–activity relationships of aroylhydrazone chelators are described that will be useful in designing new ligands or fine-tuning the activity of others, including toxic Fenton-derived free radicals.



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