Synthetic and natural products as iron chelators

Sharpe, Philip C., Richardson, Des R., Kalinowski, Danuta S. and Bernhardt, Paul V. (2011) Synthetic and natural products as iron chelators. Current Topics in Medicinal Chemistry, 11 5: 591-607. doi:10.2174/156802611794785163

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Author Sharpe, Philip C.
Richardson, Des R.
Kalinowski, Danuta S.
Bernhardt, Paul V.
Title Synthetic and natural products as iron chelators
Journal name Current Topics in Medicinal Chemistry   Check publisher's open access policy
ISSN 1568-0266
Publication date 2011-03
Sub-type Article (original research)
DOI 10.2174/156802611794785163
Volume 11
Issue 5
Start page 591
End page 607
Total pages 17
Place of publication Bussum, Netherlands
Publisher Bentham Science Publishers
Collection year 2012
Language eng
Formatted abstract
An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administration of chelators for Fe over-load aims to generate Fe complexes in vivo that are able to be excreted. Hence, the chemical and pharmacological properties of the complexes formed are as equally important as the chelators themselves. The redox properties of the Fe complexes formed are particularly relevant to their toxicity. If both FeII and FeIII oxidation states of the complexes are biologi-cally accessible, then there is potential for the catalytic production of deleterious free radicals by Fenton-type chemistry. In addition, since the burden of Fe overload disease falls predominantly on some of the poorest economies, the cost of a drug must be considered, as well as the mode of delivery. There are also possible issues with the use of naturally occurring ligands, which may form Fe complexes capable of being utilised by opportunistic bacteria. This review will concen-trate on recent developments in our chemical understanding of existing chelators approved or proposed for use and will also consider some of the candidates from natural sources that have been recently proposed.
Keyword Deferasirox
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2012 Collection
School of Chemistry and Molecular Biosciences
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Citation counts: TR Web of Science Citation Count  Cited 12 times in Thomson Reuters Web of Science Article | Citations
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Created: Thu, 16 Feb 2012, 15:34:19 EST by Lucy O'Brien on behalf of School of Chemistry & Molecular Biosciences