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Accession Number
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DE2012-1048306
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Title
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Multidentate Terephthalamidate and Hydroxypyridonate Ligands: Towards New Orally Active Chelators.
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Publication Date
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2011
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Media Count
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24p
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Personal Author
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K. N. Raymond R. J. Abergel
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Abstract
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The limitations of current therapies for the treatment of iron overload or radioisotope contamination have stimulated efforts to develop new orally bioavailable iron and actinide chelators. Siderophore-inspired tetradentate, hexadentate and octadentate terephthalamidate and hydroxypyridonate ligands were evaluated in vivo as selective and efficacious iron or actinide chelating agents, with several metal loading and ligand assessment procedures, using (sup 59)Fe, (sup 238)Pu, and (sup 241)Am as radioactive tracers. The compounds presented in this study were compared to commercially available therapeutic sequestering agents (deferoxamine (DFO) for iron and diethylenetriaminepentaacetic acid (DPTA) for actinides) and are unrivaled in terms of affinity, selectivity and decorporation efficacy, which attests to the fact that high metal affinity may overcome the low bioavailability properties commonly associated to multidenticity.
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Keywords
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Actinides
Affinity
Chelating agents
Contamination
Deferoxamine
DTPA
In vivo
Iron
Ligands
Radioisotopes
Therapy
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Source Agency
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Technical Information Center Oak Ridge Tennessee
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NTIS Subject Category
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57E - Clinical Medicine
57V - Radiobiology
99E - Photochemistry and Radiation Chemistry
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Corporate Author
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Lawrence Berkeley Lab., CA. Earth Sciences Div.
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Document Type
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Technical report
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Title Note
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N/A
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NTIS Issue Number
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1304
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Contract Number
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DE-AC02-05CH11231
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