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Design, synthesis, and physicochemical and biological characterization of a new iron chelator of the family of hydroxychromenes.

Abstract：

:Increasing evidence suggests that iron plays an important role in tissue damage both during chronic iron overload diseases (i.e., hemochromatosis) and when, in the absence of actual tissue iron overload, iron is delocalized from specific carriers or intracellular sites (inflammation, neurodegenerative diseases, postischaemic reperfusion, xenobiotic intoxications, etc.). In the present work, we appropriately modified an iron chelator of the hydroxychromene family in order to obtain a tridentate chelator that would inactivate the iron redox cycle after its complexation, with a view to using this molecule in human therapy and/or in disease prevention. We synthesized such a chelator for the first time and show, by different physicochemical analysis, its tridentate nature and, importantly, its capacity to chelate iron with enough strength to inhibit both iron-dependent H(2)O(2) generation and lipid peroxidation in in vitro biological systems.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Ferrali M,Bambagioni S,Ceccanti A,Donati D,Giorgi G,Fontani M,Laschi F,Zanello P,Casolaro M,Pietrangelo A

doi

10.1021/jm021022u

keywords:

subject

Has Abstract

pub_date

2002-12-19 00:00:00

pages

5776-85

issue

26

eissn

0022-2623

issn

1520-4804

pii

jm021022u

journal_volume

45

pub_type

杂志文章

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