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Heading the list of the critical health-related issues worldwide, cancer continues to be a one of the most serious life-threatening diseases. The rate of cancer-related mortality is at alarming level globally because of poor ability of prevention, diagnosis and efficient treatment of cancers. Pertaining to its wide prevalence in many naturally occurring compounds, coumarin as a privileged scaffold is endowed with outstanding anticancer profile. Different classes of coumarin-based anticancer agents that act through diverse mechanisms of action have been comprehensively investigated by many researchers, such as alkylating agents, topoisomerase inhibitors, hormone antagonists, angiogenesis inhibitors, antimitotic agents, apoptosis inducers, human carbonic anhydrase inhibitors, telomerase inhibitors and other mechanisms. Accordingly, medicinal chemists and drug design scientists embarked on exploring diverse …