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A synthetic molecule targeting STAT3 against human oral squamous cell carcinoma cells

Li-Yuan Bai1,2, Eman M E Dokla3, Po-Chen Chu4

  • 1Division of Hematology and Oncology, Department of Internal Medicine, China Medical University Hospital, Taichung 404, Taiwan.

International Journal of Medical Sciences
|March 3, 2025
PubMed

Insights

A synthetic molecule, N-[3-chloro-4-[5-[3-[[[4-[(cyclopropylcarbonyl)-amino]3-(trifluoromethyl)phenylamino]carbonyl]amino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]-3-pyridine-carboxamide (COC), shows potent anti-proliferative activity against oral squamous cell carcinoma (OSCC). COC induces apoptosis and inhibits migration, suggesting its potential as a novel oral cancer therapeutic.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Oral squamous cell carcinoma (OSCC) is a prevalent cancer in Taiwan requiring novel therapeutic strategies.
  • Existing treatments for OSCC have limitations, necessitating the development of new agents.

Purpose of the Study:

  • To investigate the anti-proliferative effects of the synthetic molecule N-[3-chloro-4-[5-[3-[[[4-[(cyclopropylcarbonyl)-amino]3-(trifluoromethyl)phenylamino]carbonyl]amino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]-3-pyridine-carboxamide (COC) on OSCC cells.
  • To elucidate the molecular mechanisms underlying COC's anti-cancer activity in OSCC.

Main Methods:

  • In vitro assessment of COC's anti-proliferative activity using IC50 values in OSCC cell lines (SCC2095 and SCC4).
  • Analysis of apoptosis induction via caspase activation.
  • Evaluation of signaling pathway modulation, including MAPK and STAT3.
  • Assessment of effects on cell migration and expression of E-cadherin and β-catenin.

Main Results:

  • COC demonstrated significant tumor-suppressive efficacy with low nanomolar IC50 values in OSCC cells.
  • COC induced caspase-dependent apoptosis and downregulated the MAPK signaling pathway.
  • COC modulated E-cadherin and β-catenin levels, inhibited cell migration, and decreased p-STAT3 levels.
  • STAT3 overexpression partially counteracted COC's cytotoxic effects.

Conclusions:

  • The synthetic molecule COC exhibits potent anti-proliferative and tumor-suppressive properties against OSCC.
  • COC exerts its effects through induction of apoptosis, modulation of key signaling pathways (MAPK, STAT3), and inhibition of cell migration.
  • COC represents a promising novel therapeutic agent for oral cancer treatment.
Keywords:
MAPKOral squamous cell carcinomaSTAT3apoptosismigration

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