title: Chemical features of in use and in progress chelators for iron overload.
abstract: An excessive amount of iron may become extremely toxic both for its ability to generate reactive oxygen species, and for the lack of regulatory mechanisms for iron excretion in humans. Chelation therapy has been introduced in clinical practice in the 1970's to defend thalassemia patients from the effects of iron overload and it has dramatically changed both life expectancy and quality of life. The disadvantages of the drugs in clinical use make the research for new, more suitable iron chelating agents, urgent. This review defines the requirements of an iron chelator, then points out the principal chemical features of the iron chelators in use. Finally, a survey on the last ten years of the literature relative to iron chelators is done, and the most interesting ligands are presented, with particular emphasis to those that reached clinical trials.
authors.affiliation: Department of Chemical and Geological Sciences, University of Cagliari, Cittadella Universitaria, 09042 Monserrato-Cagliari, Italy. Electronic address: nurchi@unica.it.
authors.forename: Valeria Marina
authors.initials: VM
authors.lastname: Nurchi
authors.affiliation: Department of Chemical and Geological Sciences, University of Cagliari, Cittadella Universitaria, 09042 Monserrato-Cagliari, Italy.
authors.forename: Guido
authors.initials: G
authors.lastname: Crisponi
authors.affiliation: Department of Chemical and Geological Sciences, University of Cagliari, Cittadella Universitaria, 09042 Monserrato-Cagliari, Italy.
authors.forename: Joanna I
authors.initials: JI
authors.lastname: Lachowicz
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
authors.forename: Serenella
authors.initials: S
authors.lastname: Medici
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Peana
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
authors.forename: Maria Antonietta
authors.initials: MA
authors.lastname: Zoroddu
mesh_terms: D015913:Chelation Therapy; D006801:Humans; D007502:Iron Chelating Agents / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D019190:Iron Overload / Q000188:drug therapy* / Q000378:metabolism
chemical_list: D007502:Iron Chelating Agents
keywords: Beta-thalassemia; Iron chelating agents; Kojic acid derivatives; Pyridinones; pFe