Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ 85721, United States.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):458-60. doi: 10.1016/j.bmcl.2009.11.130. Epub 2009 Dec 1.
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.
我们合成并评价了新型特异性三齿铁(III)鳌合剂 2,6-双[羟氨基]-1,3,5-三嗪(BHT)家族,用于铁剥夺癌症治疗。BHT 鳌合剂的物理性质很容易定制,便于穿透细胞膜。新型 BHT 鳌合剂的抗增殖活性在 MDA-MB-231 和 MiaPaCa 细胞上进行了研究,并与临床可用的新型口服铁鳌合剂地拉罗司(DFX)进行了比较。新型鳌合剂的抗增殖活性与铁(III)鳌合能力相关,一些类似物的抗增殖活性明显高于 DFX。