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

被引：15

作者：

Sun, Daekyu ^{[2
]}

Melman, Galina ^{[1
]}

LeTourneau, Nickolas J. ^{[1
]}

Hays, Allison M. ^{[2
]}

Melman, Artem ^{[1
]}

机构：

[1] Clarkson Univ, Dept Chem & Biomol Sci, Potsdam, NY 13699 USA

[2] Univ Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 02期

关键词：

Iron; Chelation; DFO; DFX; Cancer; Antiproliferative; Cytotoxic; Hydroxylamine; Hydroxamate; Triazine; RIBONUCLEOTIDE REDUCTASE; CANCER; TRANSFERRIN; THERAPY; DESFERRIOXAMINE; INHIBITION; APOPTOSIS; LIGANDS; AGENTS; ALPHA;

D O I：

10.1016/j.bmcl.2009.11.130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：458 / 460

页数：3

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