Work

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

Year: 2025

Type: article

Abstract: 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.

Source: Chemical Biology & Drug Design

DOI: 10.1111/cbdd.70078

Authors: Burak Kuzu, Derya Yetkin, Ceylan Hepokur, Oztekin Algul

Institutions: Van Yüzüncü Yıl Üniversitesi, Mersin Üniversitesi, Sivas Cumhuriyet Üniversitesi, Erzincan Binali Yıldırım University

Language: English

Topic: Synthesis and biological activity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $3,920