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.

Equipe de Synthèse de Molécules à Objectif Thérapeutique Laboratoire des Produits Naturels d'Origine Végétale et de Synthèse Organique Faculté des Sciences Exactes Campus de Chaabat Ersas Université Frères Mentouri Constantine1 Constantine Algeria

Faculty of Pharmacy Charles University Hradec Králové Czech Republic

LAQV REQUIMTE and Department of Chemistry University of Aveiro Aveiro Portugal

REQUIMTE LAQV Laboratório de Farmacognosia Departamento de Química Faculdade de Farmácia Universidade do Porto Porto Portugal

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