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Biological activity and molecular docking studies of some new quinolines as potent anticancer agents

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Abstract

The objective of this study is to investigate the antiproliferative and cytotoxic properties and the action mechanism of substituted quinoline and tetrahydroquinolines 3, 4, 5, 7, and 8 against rat glioblastoma (C6), human cervical cancer (HeLa), human adenocarcinoma (HT29) cancer cell lines by BrdU Cell Proliferation ELISA, Lactate Dehydrogenase, DNA laddering and Topoisomerase I assays. The results of the study showed that 6,8-dibromotetrahydroquinoline 3 possess in vitro antiproliferative activity against C6, HeLa, and HT29 cell lines while morpholine/piperazine substituted quinoline 7 and 8 showed selective antiproliferative activity on C6 cell line with IC50 values 47.5 and 46.3 µg/mL, respectively. Moreover, 6,8-dibromoTHQ 3 caused DNA fragmentation while it did not inhibit the Topoisomerase I (Topo I) enzyme. On the other hand, compound 8 did not cause DNA laddering while 8 inhibited the Topo I enzyme. According to these results, 6,8-dibromoTHQ 3 stimulates apoptosis on the C6 cell line while 6,8-dibromo-3-morhonilylquinoline (8) inhibits the Topo I enzyme to cause antiproliferative activity.

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Funding

This study was supported financially by the Scientific and Technological Research Council of Turkey (TÜBİTAK; 112T394).

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Authors and Affiliations

  1. Hamidiye Vocational School of Health Services, Department of Medical Services and Techniques, Medical Laboratory Techniques, University of Health Sciences, Üsküdar, Istanbul, Turkey

    Tuğba Kul Köprülü

  2. Faculty of Education, Department of Maths and Science Education, Division of Science Education, Kırıkkale University, Yahşihan, Kırıkkale, Turkey

    Salih Ökten

  3. Health Services Vocational School, Department and Plant and Animal Production, Medicinal and Aromatic Plants, Üsküdar University, Üsküdar, Istanbul, Turkey

    Vildan Enisoğlu Atalay

  4. Hamidiye Faculty of Medicine, Department of Basic Medical Sciences, Medical Biology, University of Health Sciences, Üsküdar, Istanbul, Turkey

    Şaban Tekin

  5. Faculty of Arts and Design, Department of Gastronomy, Istanbul Rumeli University, Silivri, 34570, Istanbul, Turkey

    Osman Çakmak

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  1. Tuğba Kul Köprülü
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  2. Salih Ökten
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  3. Vildan Enisoğlu Atalay
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  5. Osman Çakmak
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All authors were involved in research design and data collection. Köprülü and Ökten conducted data analysis and drafted manuscripts. Tekin and Çakmak revised the manuscript.

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Correspondence to Tuğba Kul Köprülü or Salih Ökten.

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Köprülü, T.K., Ökten, S., Atalay, V.E. et al. Biological activity and molecular docking studies of some new quinolines as potent anticancer agents. Med Oncol 38, 84 (2021). https://doi.org/10.1007/s12032-021-01530-w

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