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Synthesis, Biological Evaluation and In Silico Studies of Some 2-Substituted Benzoxazole Derivatives as Potential Anticancer Agents to Breast CancerKuzu, BurakHepokur, CeylanAlagoz, Mehmet AbdullahBurmaoglu, SerdarAlgul, Oztekinanticancer activitybenzoxazoleCOX inhibitioncytotoxic activitymolecular dockingCELL-CYCLEANTIOXIDANT STATUSTHALIDOMIDEINFLAMMATIONINHIBITORSDRUGCYCLOOXYGENASE-2PROGRESSIONCELECOXIBChemistry, MultidisciplinaryChemistryIn 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 μM) and compound 31 (IC50=5.82 μM) have similar activity to reference drug 5-FU (IC50=3.95 μM) 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. © 2022 Wiley-VCH GmbHJohn Wiley and Sons Inc2022Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/12963https://doi.org/10.1002/slct.2021035592365-6549enChemistrySelectinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/12963