Abstract
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. Graphic abstract: [Figure not available: see fulltext.].
| Original language | English |
|---|---|
| Article number | 84 |
| Journal | Medical Oncology |
| Volume | 38 |
| Issue number | 7 |
| DOIs | |
| Publication status | Published - Jul 2021 |
| Externally published | Yes |
Bibliographical note
Publisher Copyright:© 2021, Springer Science+Business Media, LLC, part of Springer Nature.
Keywords
- Anticancer activity
- Cytotoxicity
- Molecular docking
- Quinoline
- Tetrahydroquinoline
