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  2. Pyrrole-Tethered Bisbenzoxazole Derivatives: Apoptosis-Inducing Agents Targeting Breast Cancer Cells

Pyrrole-Tethered Bisbenzoxazole Derivatives: Apoptosis-Inducing Agents Targeting Breast Cancer Cells

  • Chem Biol Drug Des. 2025 Mar;105(3):e70078. doi: 10.1111/cbdd.70078.
Burak Kuzu 1 Derya Yetkin 2 Ceylan Hepokur 3 Oztekin Algul 4 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Van Yuzuncu Yil University, Van, Türkiye.
  • 2 Advance Technology Education Research and Application Centre, Mersin University, Mersin, Türkiye.
  • 3 Department of Biochemistry, Faculty of Pharmacy, Sivas Cumhuriyet University, Sivas, Türkiye.
  • 4 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, Türkiye.
  • 5 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Erzincan Binali Yildirim University, Erzincan, Türkiye.
Abstract

This study presents the design, synthesis, and biological evaluation of a series of novel pyrrole-tethered bisbenzoxazole (PTB) derivatives as potential apoptosis-inducing agents targeting the MCF-7 human breast Cancer cell line. The Anticancer activity of these compounds was evaluated in vitro using the MTT assay, with tamoxifen serving as the reference therapeutic agent. Compounds B8, B14, and B18 demonstrated remarkable cytotoxicity against MCF-7 cells, exhibiting approximately 8-fold lower IC50 values compared to tamoxifen, while showing minimal effects on healthy fibroblasts. Further investigations revealed that these compounds effectively induced early-stage Apoptosis and selectively arrested the cell cycle at the G1 phase in Cancer cells. Gene expression analysis confirmed selective activation of the caspase-9-mediated apoptotic pathway in MCF-7 cells, providing insights into their underlying molecular mechanisms. These findings highlight the promising potential of PTB derivatives as potent Anticancer agents, laying the groundwork for the development of targeted therapies for breast Cancer that leverage Apoptosis induction for improved therapeutic outcomes.

Keywords

Bisbenzoxazole; MTT; apoptosis; cell cycle; cytotoxicity; pyrrole; synthesis.

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