Kuzu, BurakHepokur, CeylanAlagoz, Mehmet AbdullahBurmaoglu, SerdarAlgul, Oztekin2025-05-102025-05-1020222365-654910.1002/slct.2021035592-s2.0-85123714948https://doi.org/10.1002/slct.202103559https://hdl.handle.net/20.500.14720/14250Kuzu, Burak/0000-0002-7305-7177; Hepokur, Ceylan/0000-0001-6397-1291In 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.eninfo:eu-repo/semantics/closedAccessAnticancer ActivityBenzoxazoleCox InhibitionCytotoxic ActivityMolecular DockingArticle71Q3Q3WOS:000753977300002