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

The objective of this study is to investigate the antiproliferative and cytotoxic properties and the  action mechanism of substituted quinoline and tetrahydroquinolines3,4,5,7, and8 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-dibromotetrahydroquinoline3 possess in vitro antiproliferative activity against C6, HeLa, and HT29 cell lines while morpholine/piperazine substituted quinoline7 and8 showed selective antiproliferative activity on C6 cell line with IC50 values 47.5 and 46.3  µg/mL, respectively. Moreover, 6,8-dibromoTHQ3 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 while8 inhibited the Topo I enzyme. According to these results, 6,8-dibromoTHQ3 stimulates apoptosis on the C6 cell line while 6,8-dibromo-3-morhonilylquinoline (8) inhibits the Topo I enzyme to cause antiproliferative activity.Graphic abstract
Source: Medical Oncology - Category: Cancer & Oncology Source Type: research