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Quinoline is a versatile pharmacophore, a privileged scaffold and an outstanding fused heterocyclic compound with a wide range of pharmacological prospective such as anticancer, anti-inflammatory, antibacterial, antiviral drug and superlative moiety in drug discovery. The quinoline hybrids have already been shown excellent results with new targets with a different mode of actions as an inhibitor of cell proliferation by cell cycle arrest, apoptosis, angiogenesis, disruption of cell migration and modulation. This review emphasized the mode of action, structure activity relationship and molecular docking to reveal the various active pharmacophores of quinoline hybrids accountable for novel anticancer, anti-inflammatory, antibacterial and miscellaneous activities. Therefore, several quinoline candidates are under clinical trials for the treatment of certain diseases, for example ferroquine (antimalarial), dactolisib …