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

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dc.authoridYildirim, Metin/0000-0003-1346-312X
dc.authoridTÜRKMENOĞLU, BURÇİN/0000-0002-5770-0847
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authorwosidYildirim, Metin/JMP-9922-2023
dc.authorwosidTÜRKMENOĞLU, BURÇİN/ABG-4951-2020
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
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.accessioned2024-08-04T20:53:35Z
dc.date.available2024-08-04T20:53:35Z
dc.date.issued2023
dc.departmentİnönü Üniversitesien_US
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.en_US
dc.description.sponsorshipMersin University [BAP- SBE-2020-1-TP3-4028]en_US
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.en_US
dc.identifier.doi10.1016/j.molstruc.2023.135513
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85151795059en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2023.135513
dc.identifier.urihttps://hdl.handle.net/11616/101275
dc.identifier.volume1285en_US
dc.identifier.wosWOS:000980922000001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofJournal of Molecular Structureen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBenzazoleen_US
dc.subjectSynthesisen_US
dc.subjectMTTen_US
dc.subjectBreast canceren_US
dc.subjectAntiproliferativeen_US
dc.subjectHuman DNA topoisomerase II ?en_US
dc.subjectMolecular dockingen_US
dc.subjectADMEen_US
dc.titleN-(benzazol-2-yl)-2-substituted phenylacetamide derivatives: Design, synthesis and biological evaluation against MCF7 breast cancer cell lineen_US
dc.typeArticleen_US

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