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Synthesis of novel quinoline-thiazolobenzimidazolone hybrids as anticancer agents through caspase-dependent apoptosis
H. Bouria, H. Alliouche, MI. Chouiter, A. Belfaitah, T. Pacheco, V. Gala, D. Pereira, AMS. Silva
Language English Country England, Great Britain
Document type Journal Article
- MeSH
- Apoptosis * drug effects MeSH
- Benzimidazoles * pharmacology chemistry chemical synthesis MeSH
- Quinolines * chemistry pharmacology chemical synthesis MeSH
- Caspases * metabolism MeSH
- Humans MeSH
- Molecular Structure MeSH
- Cell Line, Tumor MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents * pharmacology chemistry chemical synthesis MeSH
- Drug Screening Assays, Antitumor MeSH
- Molecular Docking Simulation * MeSH
- Thiazoles chemistry pharmacology chemical synthesis MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
AIM: This work explores the synthesis of new bi-heterocyclic hybrid compounds based on quinoline ring and investigates their potential as anticancer agents. MATERIALS & METHODS: The novel fused quinoline-thiazolo[3,2-a] benzimidazole-3(2 h)one hybrids were prepared by regioselective nucleophilic ring opening of the corresponding quinolinyl-oxiranes. In vitro cytotoxic activity was evaluated against human lung (A549) and gastric (AGS) cancer cell lines. RESULTS: Global results showed that all tested compounds have promising inhibitory properties. Compounds 17 and 18 bearing two methoxy groups on the quinoline ring have exhibited remarkable and interesting activities. The investigation of the cell death process showed that these compounds activated a caspase-dependent apoptosis pathway. Results were further supported by molecular docking studies. CONCLUSION: Both compounds exhibited good drug-like characteristics, which make them promising drug candidates.
Faculty of Pharmacy Charles University Hradec Králové Czech Republic
LAQV REQUIMTE and Department of Chemistry University of Aveiro Aveiro Portugal
References provided by Crossref.org
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