1. Academic Validation
  2. Synthesis and antiproliferating activity of iron chelators of hydroxyamino-1,3,5-triazine family

Synthesis and antiproliferating activity of iron chelators of hydroxyamino-1,3,5-triazine family

  • Bioorg Med Chem Lett. 2010 Jan 15;20(2):458-60. doi: 10.1016/j.bmcl.2009.11.130.
Daekyu Sun 1 Galina Melman Nickolas J Letourneau Allison M Hays Artem Melman
Affiliations

Affiliation

  • 1 Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ 85721, United States.
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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