Iron Chelators and Therapeutic Applications

Iron chelators are specialised molecules that bind free iron ions, forming stable complexes amenable to safe excretion or redistribution. Their development has revolutionised the treatment of iron‐overload disorders such as thalassaemia and haemochromatosis, where organ damage arises from excess ferric (Fe3+) deposition. Beyond classic chelation therapy, advances in ligand design have yielded multifunctional agents capable of selective delivery to diseased tissues, neuroprotective action in iron‐mediated neurodegeneration and adjunct antimicrobial strategies that starve pathogens of essential metal ions. Synthetic scaffolds range from hexadentate hydroxypyridinones to triazamacrocycles and hybrid bioinspired derivatives modelled on natural iron‐binding molecules. Optimisation of denticity, lipophilicity and redox stability has enabled oral administration, targeted cellular uptake and compatibility with imaging isotopes. Emerging applications encompass radiopharmaceuticals for positron emission tomography, colourimetric assays for environmental monitoring and tailored therapies addressing oxidative stress in Parkinson’s and Alzheimer’s disease. The global significance of iron chelation lies in its capacity to mitigate iron‐driven pathology across diverse clinical contexts, while ongoing research seeks biodegradable, high‐affinity ligands that preserve essential metal homeostasis and support precision medicine approaches.

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Iron Chelators and Therapeutic Applications publication trend

The graph below shows the total number of articles in iron chelators and therapeutic applications across all publications each year (not limited to Nature Index journals).

Technical terms

Chelator: A molecule that binds metal ions through multiple coordinating atoms to form a stable complex.

Ferric complex: A coordination compound in which iron is in the +3 oxidation state.

Hydroxypyridinone: A chelating moiety based on a pyridinone ring bearing hydroxyl groups for high‐affinity metal binding.

Denticity: The number of donor atoms in a ligand that coordinate to a single metal centre.

Radiopharmaceutical: A compound labelled with a radionuclide for diagnostic imaging or therapeutic applications.

Redox stability: The resistance of a metal–ligand complex to oxidation or reduction under physiological conditions.

References

1. Multipurpose Iron-Chelating Ligands Inspired by Bioavailable Molecules. Biomolecules (2024).
2. Amphetamine-like Deferiprone and Clioquinol Derivatives as Iron Chelating Agents. Molecules (2024).
3. Hydroxypyridinone Chelators: From Iron Scavenging to Radiopharmaceuticals for PET Imaging with Gallium-68. International Journal of Molecular Sciences (2017).
4. One-step determination of total iron using deferiprone or kojic acid as colorimetric reagents. Results in Chemistry (2024).
5. Synthesis of novel Iron(III) chelators based on triaza macrocycle backbone and 1-hydroxy-2(H)-pyridin-2-one coordinating groups and their evaluation as antimicrobial agents. Journal of Inorganic Biochemistry (2016).
6. Recent developments centered on orally active iron chelators. Thalassemia Reports (2014).