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

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dc.contributor.authorKuzu, Burak
dc.contributor.authorYetkin, Derya
dc.contributor.authorHepokur, Ceylan
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2025-05-04T16:46:52Z
dc.date.available2025-05-04T16:46:52Z
dc.date.issued2025
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractThis 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.
dc.description.sponsorshipVan YYU BAP; [FDK-TYD-2022-9949]
dc.description.sponsorshipThis work was supported by Van YYU BAP (Project code: FDK-TYD-2022-9949).
dc.identifier.doi10.1111/cbdd.70078
dc.identifier.issn1747-0277
dc.identifier.issn1747-0285
dc.identifier.issue3
dc.identifier.pmid40079412
dc.identifier.scopus2-s2.0-105000330326
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1111/cbdd.70078
dc.identifier.urihttps://hdl.handle.net/20.500.12418/35374
dc.identifier.volume105
dc.identifier.wosWOS:001443352600001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofChemical Biology & Drug Design
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WOS_20250504
dc.subjectapoptosis
dc.subjectBisbenzoxazole
dc.subjectcell cycle
dc.subjectcytotoxicity
dc.subjectMTT
dc.subjectpyrrole
dc.subjectsynthesis
dc.titlePyrrole-Tethered Bisbenzoxazole Derivatives: Apoptosis-Inducing Agents Targeting Breast Cancer Cells
dc.typeArticle

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