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Lysosome-Targeted Squaramide Anion Transporters

Elba Feo1, Edward York1,2, Anthony Thai1

  • 1School of Mathematical and Physical Sciences, Faculty of Science, University of Technology Sydney, Sydney, New South Wales, Australia.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|June 9, 2026
PubMed

Insights

New squaramide anion transporters were synthesized and targeted to cancer cell lysosomes. The N,N-dimethylamine group enhanced cytotoxicity more than other targeting groups, showing promise for cancer therapy.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Molecular Pharmacology

Background:

  • Targeting specific organelles enhances the efficacy of cytotoxic agents against cancer cells.
  • Anion transporters are potential targets for cancer therapy.
  • Lysosomes are key organelles for cellular degradation and drug delivery.

Purpose of the Study:

  • To synthesize novel squaramide anion transporters.
  • To append lysosome-targeting groups to these transporters.
  • To evaluate their cytotoxicity and subcellular localization in cancer cell lines.

Main Methods:

  • Synthesis of squaramide derivatives with N,N-dimethylamine and morpholine targeting groups.
  • Cell viability assays (e.g., MTT assay) to determine cytotoxicity.
  • Subcellular localization studies using fluorescence microscopy with anthracene-labeled compounds.

Main Results:

  • Squaramide transporters with the N,N-dimethylamine targeting group showed the highest cytotoxicity.
  • Cytotoxicity was observed despite lower transport activity compared to non-targeted controls.
  • Both targeting groups successfully directed compounds to lysosomes, with N,N-dimethylamine showing greater accumulation.

Conclusions:

  • Lysosome-targeting via N,N-dimethylamine enhances the anticancer activity of squaramide anion transporters.
  • The N,N-dimethylamine moiety represents a promising strategy for developing targeted cancer therapeutics.
  • Further investigation into the mechanism of action is warranted.
Keywords:
anion bindinganion transportlysosome‐targetingsquaramidessupramolecular chemistry

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