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  • Küçük Resim
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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.
  • Küçük Resim
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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.