Köprülü, Tuğba KulÖkten, SalihAtalay, Vildan EnisogluTekin, ŞabanÇakmak, Osman2025-01-212025-01-2120211357-05601559-131Xhttps://doi.org/10.1007/s12032-021-01530-whttps://hdl.handle.net/20.500.12587/24274The 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 mu g/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. Graphic abstracteninfo:eu-repo/semantics/openAccessQuinoline; Tetrahydroquinoline; Anticancer activity; Cytotoxicity; Molecular dockingArticle38710.1007/s12032-021-01530-w2-s2.0-8510814131534146171Q2WOS:000691898600001Q3