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Coumarin derivatives have progressively enticed medicinal chemists because of their potential role in preventing and treating ailments. They epitomize a key motif nucleus in heterocyclic chemistry and a privileged structure in medicinal chemistry because of its extensive-range pharmacological activity. Regardless of the advancement in medicine over the past century, cancer is still remain the prominent source of death in the world and it makes indispensible needs to synthesize the compounds with coumarin as the core nucleus. Synthesis of various coumarin derivatives and evaluation of their pharmacological effects can perceive a solution to certain enigmatic demands in health sector. This review article is fixated on different synthetic routes of coumarin nucleus containing compounds. The review article also highlights different biological activities such as anticancer, antibacterial, anti- inflammatory, antihyperlipidemic and enzyme inhibition activities.