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

Daekyu Sun, Galina Melman, Nickolas J. LeTourneau, Allison M. Hays, Artem Melman

Research output: Contribution to journalArticle

12 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)458-460
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number2
DOIs
StatePublished - Jan 15 2010

Fingerprint

Triazines
Chelating Agents
Iron
Butylated Hydroxytoluene
Chelation
Physical properties
Membranes
Neoplasms

Keywords

  • Antiproliferative
  • Cancer
  • Chelation
  • Cytotoxic
  • DFO
  • DFX
  • Hydroxamate
  • Hydroxylamine
  • Iron
  • Triazine

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Synthesis and antiproliferating activity of iron chelators of hydroxyamino-1,3,5-triazine family. / Sun, Daekyu; Melman, Galina; LeTourneau, Nickolas J.; Hays, Allison M.; Melman, Artem.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 2, 15.01.2010, p. 458-460.

Research output: Contribution to journalArticle

Sun, Daekyu ; Melman, Galina ; LeTourneau, Nickolas J. ; Hays, Allison M. ; Melman, Artem. / Synthesis and antiproliferating activity of iron chelators of hydroxyamino-1,3,5-triazine family. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 2. pp. 458-460.
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