An orally bioavailable iron chelator with anticancer activity; selective for (Fe(III) over Cu(II), Zn(II), Mg(II), and Ca(II) but does bind to Al(III); decreases iron levels in iron-loaded rat heart cells in vitro by 45.8 and 55.6% compared to control levels at 160 and 320 μM; decreases radiolabeled liver iron levels from 41 to 21.7% and blood iron levels from 8.2 to 3.4% in hypertransfused rats at 200 mg/kg; inhibits proliferation of SAS human oral squamous carcinoma cells (EC50 = 21 μM); act synergistically with gemcitabine in vitro to inhibit proliferation and in vivo to reduce tumor growth at 200 mg/kg in a BxPC-3 mouse xenograft model