In vitro studies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics.
Axel SteinbrueckAdam C SedgwickHai-Hao HanMichael Y ZhaoSajal SenDan-Ying HuangYi ZangJia LiXiao-Peng HeJonathan L SesslerPublished in: Chemical communications (Cambridge, England) (2021)
We report here strategic functionalization of the FDA approved chelator deferasirox (1) in an effort to produce organelle-targeting iron chelators with enhanced activity against A549 lung cancer cells. Derivative 8 was found to have improved antiproliferative activity relative to 1. Fluorescent cell imaging revealed that compound 8 preferentially localises within the lysosome.