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Preliminary evaluation of antiproliferative and apoptotic activities of novel indolin-2-one derivatives

Gulseren Turhal1, Busra Demirkan1, Izel Nermin Baslilar1

  • 1Department of Molecular Biology & Genetics, Faculty of Science, Gebze Technical University, Kocaeli, Turkey.

Drug Development Research
|July 3, 2024
PubMed

Insights

Novel indolin-2-one derivatives show potent anticancer effects by inhibiting key signaling pathways and inducing apoptosis in cancer cells. Compound 6d demonstrates broad efficacy across multiple cancer types, including breast and colon cancer.

Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Oncology

Background:

  • Indole-based compounds are vital in cancer therapy.
  • Novel indolin-2-one derivatives were synthesized for evaluation.

Purpose of the Study:

  • To investigate the anticancer properties of novel indolin-2-one derivatives (6a-d).
  • To assess their efficacy against Malignant Mesothelioma, Breast cancer, and Colon Cancer cell lines.

Main Methods:

  • Assessed inhibition of ERK1/2, AKT, and STAT3 signaling pathways.
  • Analyzed cell cycle progression and apoptosis markers (Bax, Bcl-2, p21, p27).
  • Evaluated caspase 3 activation and PARP cleavage.

Main Results:

  • All derivatives inhibited cell proliferation and induced S-phase cell cycle arrest.
  • Mitochondrial apoptosis was initiated via modulation of Bax/Bcl-2 ratio.
  • Three derivatives showed selectivity for breast and colon cancer cells, with compound 6d being the most potent.

Conclusions:

  • Novel indolin-2-one derivatives possess significant anticancer activity.
  • Compound 6d is a promising candidate for broad-spectrum cancer therapy, particularly for breast and colon cancers.
Keywords:
breast cancermalignant mesotheliomanovel indolin‐2‐one

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