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Anticancer activities of coumarins and their structure–activity relationships
(Elsevier B.V., 2025) Taban, Kevser; İlhan, Mert; Süntar, Ipek Peşin
Coumarins are naturally occurring compounds consisting of a 1,2-benzopyrone ring system. They exhibit a wide range of biological activities, including antimicrobial, antiinflammatory, antihypertensive, antihyperlipidemic, analgesic, anticoagulant, and anticancer. These compounds have attracted attention in cancer therapy by targeting a number of pathways. Among them, the main mechanism is based on cell cycle blockage and initiation of programmed cell death like apoptosis or autophagy. The recognition of the main structural features in coumarin is vital for the design and development of new analogs with enhanced activity and for the characterization of their mechanism of action and potential side effects. This chapter will highlight the key structure–activity relationships studies performed on coumarin derivates. Key structural features of the coumarin scaffold where substitutions can increase or decrease the anticancer activity of hit molecules will be discussed. © 2025 Elsevier B.V., All rights reserved.