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    Design, synthesis and in vitro antiproliferation activity of some 2-aryl and -heteroaryl benzoxazole derivatives
    (2022) Kuzu, Burak; HEPOKUR, CEYLAN; Türkmenoğlu,Burçin; Burmaoğlu,Serdar; Algül, öztekin
    Background: Phortress produces reactive electrophilic metabolites that form DNA adducts only in sensitive tumor cells. The authors converted the 2-phenylbenzothiazole nucleus in phortress to 2- aryl and -heteroaryl benzoxazole derivatives (11 new and 14 resynthesized). All synthesized compounds were studied for antitumor activity in various cancer cells. Materials & methods: Cytotoxicity, cell morphology, flow cytometry and cell-cycle analyses of compounds were performed and more active derivatives were tested in the MCF-7 cell line. Conclusion: Methyl 2- (thiophen-2-yl)benzo[d]oxazole-6-carboxylate (BK89) has a higher effect than fluorouracil to induce apoptotic cell death (apoptosis value of 49.44%). Cell-cycle analysis shows that the compounds BK89 and methyl 2-(furan-2-yl)benzo[d]oxazole-6-carboxylate (BK82) can be used as potential cell-cycle blockers by arresting MCF-7 cells in G0/G1 phase at rates of 63% and 85%, respectively.
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    Novel oxalamide derivatives for COXs expression and breast cancer: design, synthesis, biological evaluation, and docking studies
    (Acg Publications, 2023) Kuzu, Burak; Hepokur, Ceylan; Algul, Oztekin
    In the present study, new oxalamide-based compounds were designed from thalidomide and synthesized easily and with high yields (from 69% up to 93%) by a two-step method. The antiproliferative effects of synthesized 6a-d and 7a-d compounds on (ER+) MCF-7 and (ER-) MDA-MB-231 breast cancer cell line and human fibroblast WI-38 healthy cell line were investigated by the MTT method. The results showed that compound 7d was the most potent candidate against both MCF-7 and MDA-MB-231 cell lines with IC50 = 4.72 & mu;M and 6.37 & mu;M, respectively. To investigate whether antiproliferative effect of the compounds on breast cancer cell lines is dependent on COXs, expressions of COX-1/2 on the MCF-7 cell line were investigated by the Western-Blot technique. Among synthesized compounds, compound 7d increased the expression of both COX-1 and COX-2. The inhibition potential of compounds on COX-1/2 enzymes was investigated by molecular docking compared to inhibitor co-ligand celecoxib in crystal structures of COX-1 (PDB ID: 3KK6) and COX-2 (PDB ID: 3LN1). Docking results indeed showed that compound 7d had a higher binding affinity for both COX-1 and COX-2 active sites. Consequently, the novel oxalamide-based compounds presented here may be important candidate molecules for the development of new COX-dependent antiproliferative agents.& COPY;2023 ACG Publication. All right reserved.
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    Pyrrole-Tethered Bisbenzoxazole Derivatives: Apoptosis-Inducing Agents Targeting Breast Cancer Cells
    (Wiley, 2025) Kuzu, Burak; Yetkin, Derya; Hepokur, Ceylan; Algul, Oztekin
    This study presents the design, synthesis, and biological evaluation of a series of novel pyrrole-tethered bisbenzoxazole (PTB) derivatives as potential apoptosis-inducing agents targeting the MCF-7 human breast cancer cell line. The anticancer activity of these compounds was evaluated in vitro using the MTT assay, with tamoxifen serving as the reference therapeutic agent. Compounds B8, B14, and B18 demonstrated remarkable cytotoxicity against MCF-7 cells, exhibiting approximately 8-fold lower IC50 values compared to tamoxifen, while showing minimal effects on healthy fibroblasts. Further investigations revealed that these compounds effectively induced early-stage apoptosis and selectively arrested the cell cycle at the G1 phase in cancer cells. Gene expression analysis confirmed selective activation of the caspase-9-mediated apoptotic pathway in MCF-7 cells, providing insights into their underlying molecular mechanisms. These findings highlight the promising potential of PTB derivatives as potent anticancer agents, laying the groundwork for the development of targeted therapies for breast cancer that leverage apoptosis induction for improved therapeutic outcomes.
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    Synthesis, Biological Evaluation and In Silico Studies of Some 2-Substituted Benzoxazole Derivatives as Potential Anticancer Agents to Breast Cancer
    (Wiley-V C H Verlag Gmbh, 2022) Kuzu, Burak; Hepokur, Ceylan; Alagoz, Mehmet Abdullah; Burmaoglu, Serdar; Algul, Oztekin
    In 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.
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    Synthesis, Biological Evaluation and In Silico Studies of Some 2?Substituted Benzoxazole Derivatives as Potential Anticancer Agents to Breast Cancer
    (2022) Kuzu, Burak; HEPOKUR, CEYLAN; Alagöz, Mehmet Abdullah; Burmaoğlu,Serdar; Algül, öztekin
    In an attempt to develop potent and selective anticancer agents, some 5- or 6- and N-substituted benzoxazol-2-carbox amide 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.