Abstract Cinnoline is an innovative heterocyclic compound containing a six-membered ring fused with two nitrogen atoms. Cinnoline derivatives exhibited diverse pharmacological properties like anti-bacterial, anti-fungal,anti-parasitic, anti-inflammatory,anti-tubercular, and anti-cancer activity. In the current study, we have concentrated on the numerous biological functions and targets of cinnoline derivatives that have been studied by researchers over the last 15 years. This literature review will surely serve as the beginning point for further research and the creation of new cinnoline-based compounds with optimized properties.