Synthesis, Biological Evaluation and In Silico Studies of Some 2-Substituted Benzoxazole Derivatives as Potential Anticancer Agents to Breast Cancer

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dc.authoridKUZU, Burak/0000-0002-7305-7177
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridKUZU, Burak/0000-0002-7305-7177
dc.authoridhepokur, ceylan/0000-0001-6397-1291
dc.authorwosidKuzu, Burak/AFQ-0493-2022
dc.authorwosidKUZU, Burak/AAE-1597-2022
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.authorwosidKUZU, Burak/GVS-6838-2022
dc.contributor.authorKuzu, Burak
dc.contributor.authorHepokur, Ceylan
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2024-08-04T20:51:37Z
dc.date.available2024-08-04T20:51:37Z
dc.date.issued2022
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn an attempt to develop potent and selective anticancer agents, some 5- or 6- and N-substituted benzoxazol-2-carboxamide derivatives were designed, synthesized, and evaluated for their cyclooxygenase inhibitory, antioxidant, and anti-proliferative activity against MCF-7 and MDA-MB-231 cell lines. Among them 5-OMe, N-piperidine substituted (compound 30), 5-OMe, N-4-methylpiperidine substituted (compound 31) and 5-Cl, N-piperidine substituted (compound 34) benzoxazole 2-carboxamide compounds have a moderate inhibitory effect in COX-1 and COX-2 enzymes. Anti-proliferative studies show that compound 30 (IC50=5.35 mu M) and compound 31 (IC50=5.82 mu M) have similar activity to reference drug 5-FU (IC50=3.95 mu M) on MCF-7 cell but they have lower toxic effect for healthy WI-38 cell line. For the MCF-7 cell line, compounds 30 and 31 show approximately 1.5 times higher selectivity compared to the 5-FU control. Among the synthesized compounds 30, 31, and 34 had the best anti-proliferative effect and were used to perform flow cytometry and cell cycle analysis on MCF-7 cell line. To predict the binding modes and pharmacokinetic parameters of all compounds, in silico studies were carried out. These compounds may shed light on cancer treatment and cancer research.en_US
dc.description.sponsorshipBAP Project of Mersin University [2019-3-TP3-3806]en_US
dc.description.sponsorshipThis study was financially supported by 2019-3-TP3-3806 BAP Project of Mersin University.en_US
dc.identifier.doi10.1002/slct.202103559
dc.identifier.issn2365-6549
dc.identifier.issue1en_US
dc.identifier.scopus2-s2.0-85123714948en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/slct.202103559
dc.identifier.urihttps://hdl.handle.net/11616/100447
dc.identifier.volume7en_US
dc.identifier.wosWOS:000753977300002en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofChemistryselecten_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectanticancer activityen_US
dc.subjectbenzoxazoleen_US
dc.subjectCOX inhibitionen_US
dc.subjectcytotoxic activityen_US
dc.subjectmolecular dockingen_US
dc.titleSynthesis, Biological Evaluation and In Silico Studies of Some 2-Substituted Benzoxazole Derivatives as Potential Anticancer Agents to Breast Canceren_US
dc.typeArticleen_US

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