N-(benzazol-2-yl)-2-substituted phenylacetamide derivatives: Design, synthesis and biological evaluation against MCF7 breast cancer cell line

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dc.authoridTURKMENOGLU, BURCIN/0000-0002-5770-0847
dc.contributor.authorZoatier, Bayan
dc.contributor.authorYildirim, Metin
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorYetkin, Derya
dc.contributor.authorTurkmenoglu, Burcin
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2025-03-17T12:27:02Z
dc.date.available2025-03-17T12:27:02Z
dc.date.issued2023
dc.departmentTarsus Üniversitesi
dc.description.abstractThis work describes the straightforward and efficient one-pot synthesis of a new library of N-(benzazol-2-yl)-2-substituted phenylacetamide derivatives (19-27). Using the MTT assay, these compounds were evaluated for their in vitro anticancer activity against the MCF7 human breast cancer cell line, and the results were compared to the standard doxorubicin. The majority of compounds exhibited an inhibitory effect against the cancer cell line, with compounds 19, 22, and 26 exhibiting exceptional cytotoxicity against MCF7 cells. Using flow cytometry, the most potent compound 19 on the induction of apoptosis in the breast cancer cell line was determined. Compound 19 induced G1-phase cell cycle arrest followed by apoptotic cell death. In silico analyses of potent compounds 19, 22, and 26 were conducted to investigate their interactions with Human DNA topoisomerase II. The energy calculations were found to be in excel-lent agreement with the calculated IC50 values. In addition, drug similarity parameter values for the three active compounds were determined using in silico ADME prediction studies. Considering all of these re-sults, it appears that these N-(benzazol-2-yl)-2-substituted phenylacetamide derivatives may be effective anticancer agents. This work may possibly generate new concepts for the enhancement of inhibitors of human DNA topoisomerase II for breast cancer treatment.(c) 2023 Elsevier B.V. All rights reserved.
dc.description.sponsorshipMersin University [BAP- SBE-2020-1-TP3-4028]
dc.description.sponsorshipWe thank Mersin University for their financial support (BAP- SBE-2020-1-TP3-4028) . We are also grateful Erzincan Binali Yildirim University, Basic Sciences Application and Research Cen- ter (EBYU-EUTAM) for the Schr?dinger Maestro 2021-2 program.
dc.identifier.doi10.1016/j.molstruc.2023.135513
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85151795059
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2023.135513
dc.identifier.urihttps://hdl.handle.net/20.500.13099/2016
dc.identifier.volume1285
dc.identifier.wosWOS:000980922000001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherElsevier
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WOS_20250316
dc.subjectBenzazole
dc.subjectSynthesis
dc.subjectMTT
dc.subjectBreast cancer
dc.subjectAntiproliferative
dc.subjectHuman DNA topoisomerase II ?
dc.subjectMolecular docking
dc.subjectADME
dc.titleN-(benzazol-2-yl)-2-substituted phenylacetamide derivatives: Design, synthesis and biological evaluation against MCF7 breast cancer cell line
dc.typeArticle

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