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Updated: May 24, 2025

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Penta-1,4-dien-3-one and quinoxaline conjugates as potential anticancer agents via inhibiting EphB3/SRC/AKT axis

Qing Li1, Mei Zhou1, Ying Yang1

  • 1State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, 550014 Guiyang, PR China; Natural Products Research Center of Guizhou Province, 550014 Guiyang, PR China.

Life Sciences
|February 28, 2025
PubMed

Insights

Novel compounds targeting EphB3 show promise for hepatocellular carcinoma (HCC) treatment. Compound W8 effectively inhibits cancer cell growth and tumor progression by modulating EphB3 signaling, offering a potential new avenue for targeted cancer therapy.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • EphB3 overexpression is linked to cancer progression, making it a key therapeutic target.
  • Pharmacophore fusion strategies are employed to design novel anti-cancer agents.

Purpose of the Study:

  • To design and synthesize novel EphB3 inhibitors using pharmacophore fusion.
  • To evaluate the anti-cancer activity of these compounds against hepatocellular carcinoma (HCC).

Main Methods:

  • Synthesis of penta-1,4-dien-3-one and quinoxaline conjugates.
  • CCK-8 assays for anti-cancer activity evaluation.
  • In vivo xenograft studies in mice to assess tumor growth inhibition.

Main Results:

  • Most synthesized compounds exhibited significant anti-cancer activity against HCC.
  • Compound W8 showed potent inhibition of MHCC97H cells (IC50 = 1.87 μM), inducing G0/G1 arrest and apoptosis.
  • W8 suppressed tumor growth in vivo, reducing tumor volume and weight by down-regulating EphB3 phosphorylation and the SRC-AKT pathway.

Conclusions:

  • Compound W8 is a promising lead compound for EphB3-overexpressing cancers.
  • W8 demonstrates potential for targeted therapy in precision oncology.
  • Further drug development of W8 could offer new treatment strategies for HCC.
Keywords:
EphB3Hepatocellular carcinomaPenta-1,4-dien-3-oneQuinoxalineStructure optimization

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