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 tetrahydroquinolines 3 , 4 , 5 , 7 , and 8 against rat glioblastoma (C6), human cervical cancer (HeLa), human adenocarcinoma (HT29) cancer cell lines by...

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Bibliographic Details
Published in:Medical oncology (Northwood, London, England) London, England), 2021-07, Vol.38 (7), p.84-84, Article 84
Main Authors: Köprülü, Tuğba Kul, Ökten, Salih, Atalay, Vildan Enisoğlu, Tekin, Şaban, Çakmak, Osman
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Biological activity
Cancer therapies
Cell culture
Cell cycle
Cell growth
Cell Proliferation - drug effects
Cell Proliferation - physiology
Cervical cancer
Cytotoxicity
Dehydrogenases
Dose-Response Relationship, Drug
Enzymes
HeLa Cells
Hematology
HT29 Cells
Humans
Internal Medicine
Kinases
MCF-7 Cells
Medical research
Medicine
Medicine & Public Health
Metabolism
Metabolites
Metastasis
Molecular Docking Simulation - methods
Oncology
Original Paper
Pathology
Quinolines - chemistry
Quinolines - pharmacology
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Summary: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 IC 50 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
ISSN:1357-0560
1559-131X
DOI:10.1007/s12032-021-01530-w