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Iron Deprivation Cancer Therapy

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ironjustice

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Dec 6, 2009, 9:51:39 AM12/6/09
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Synthesis and antiproliferating activity of iron chelators
of hydroxyamino-1, 3, 5-triazine family
Bioorganic & Medicinal Chemistry Letters,
Available online 1 December 2009
Daekyu Sun, Galina Melman, Nickolas J. LeTourneau,
Allison M. Hays, Artem Melman

Abstract
We synthesized and evaluated new specific tridentate
iron(III) chelators of 2,6-bis[hydroxyamino]-1,3,5-triazine
(BHT) family for use in iron deprivation cancer therapy.
Physical properties of BHT chelators are easily customizable
allowing easy penetration through cellular membranes.
Antiproliferative activity of new BHT chelators was studied
on MDA-MB-231 and MiaPaCa cells and compared to a clinically
available new oral iron chelator, deferasirox (DFX).
The antiproliferative activity of new chelators was found to
correlate with iron(III) chelation ability and some of analogs
showed substantially higher antiproliferative activity than DFX.


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