In vitro studies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics

Axel Steinbrueck; Adam C. Sedgwick; Hai-Hao Han; Michael Y. Zhao; Sajal Sen; Dan-Ying Huang; Yi Zang; Jia Li; Xiao-Peng He; Jonathan L. Sessler

doi:10.1039/D0CC08156F

In vitro studies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics†

Axel Steinbrueck,

^a Adam C. Sedgwick,^a Hai-Hao Han,^b Michael Y. Zhao,^a Sajal Sen,

^a Dan-Ying Huang,^a Yi Zang,^c Jia Li,*^c Xiao-Peng He*^b and Jonathan L. Sessler

*^a

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* Corresponding authors

^a Department of Chemistry, University of Texas at Austin, 105 E 24th street A5300, Austin, TX 78712-1224, USA
E-mail: sessler@cm.utexas.edu

^b Key Laboratory for Advanced Materials and Joint International Research Laboratory of Precision Chemistry and Molecular Engineering, Feringa Nobel Prize Scientist Joint Research Center, Frontiers Center for Materiobiology and Dynamic Chemistry, School of Chemistry and Molecular Engineering, East China University of Science and Technology, 130 Meilong Rd., Shanghai 200237, China
E-mail: xphe@ecust.edu.cn

^c National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, P. R. China
E-mail: jli@simm.ac.cn

Abstract

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.

Chemical Communications

In vitro studies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics†

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In vitro studies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics

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