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Author Spotlight: Assessing the Impact of Novel Iron Chelators on Cancer Cell Metabolism
Published on: February 23, 2024
Synthesis and iron chelating properties of hydroxypyridinone and hydroxypyranone hexadentate ligands
Tao Zhou1, Xiao-Le Kong, Robert C Hider
1School of Food Science and Biotechnology, Zhejiang Gongshang University, 18 Xuezheng Street, Xiasha, Hangzhou, Zhejiang 310018, P. R. China. taozhou@zjgsu.edu.cn.
Abstract:
Chelation therapy has become an important therapeutic approach for some diseases. In attempt to identify clinically useful chelators, four hexadentate ligands were synthesized by conjugating the corresponding bidentate ligands (3-hydroxypyridin-4-one (3,4-HOPO), 3-hydroxypyridin-2-one (3,2-HOPO), 1-hydroxypyridin-2-one (1,2-HOPO), and 3-hydroxypyran-4-one) each with a free amino group to a tripodal acid. Their pKa values and affinities for iron(iii) were investigated. The pFe3+ values of the hexadentate pyridinones 1 (3,4-HOPO), 3 (3,2-HOPO) and 4 (1,2-HOPO), and the pyranone 2 was found to follow the sequence 1 > 4 ≫ 3 > 2, which is different to the pFe3+ value sequence of the corresponding bidentate forms (3,4-HOPO ≫ 3,2-HOPO > 1,2-HOPO > 3-hydroxypyranone). Hexadentate 3,4-HOPOs and 1,2-HOPOs have the greatest potential as iron scavenging agents.
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