Coumarin–chalcone hybrids in cancer therapy: A comprehensive review of mechanistic insights

In recent years, coumarin–chalcone hybrids have emerged as promising leads for antitumor agents, combining the distinct pharmacological profiles of coumarin and chalcone into a single molecule. The hybrids have shown multitarget activity, which affects cell cycle progression, apoptosis, oxidative stress, mitochondrial dysfunction, DNA intercalation, and angiogenesis. The results showed coumarin to be mainly involved in kinase inhibition and apoptosis, while chalcones were mainly involved in ROS production, Tubulin inhibition, and NF-κB regulation; their combination led to a synergistic effect. Despite these benefits, there are challenges and drawbacks, such as drug resistance development, hydrophobicity, instability, and possibly off-target toxicities. Current developments in nanocarriers for drug delivery systems, SAR research, and multiple target drug development approaches have remedied these challenges. In summary, available data have reinforced not only the therapeutic versatility of coumarin–chalcone hybrids but have also supported their prospective ability to serve as promising new-generation anticancer agents.

کلیدواژه ها:

Coumarin-chalcone hybrids ، anticancer activity ، Multitarget drug design ، Apoptosis ، structure-activity relationship