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May 6, 2026International Journal of Molecular SciencesOpen Access

N-Substituted-2-(9H-Xanthen-9-yl)acetamide Derivatives Induce In Vitro Colon Cancer Cell Death via TASK-1 Inhibition: Lead Compounds for Further Optimization as TASK-1-Targeted Therapeutics in Colorectal Cancer

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Authors

AKAbdulaziz H. Al KhzemSRS. M. El RayesIAIbrahim Ali

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Overview

Novel xanthene derivatives induce cell death in colon cancer, indicating potential as TASK-1-targeted treatments.

Key Points

  • This research aims to evaluate the cytotoxic effects of xanthene derivatives on colon cancer cells via TASK-1 inhibition.
  • Synthesized 27 xanthene derivatives via azide coupling and hydrazine conversion.
  • Evaluated cytotoxicity against HCT-116 cell line in vitro.
  • Conducted molecular docking and dynamics simulations to analyze protein-ligand interactions.
  • Several derivatives showed moderate cytotoxic activity with IC50 values between 66.97 and 99.62 µM.
  • Compound 7h exhibited strong antiproliferative effects, reducing cell count and causing apoptotic body formation.
  • Molecular docking revealed favorable binding of compounds within the TASK-1 potassium channel.

Cite This Study

Khzem et al. (2026) studied this question.

synapsesocial.com/papers/69fa979b04f884e66b531885https://doi.org/10.3390/ijms27094069
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