Anticancer potential of chalcones

Moi, Davide;Onnis, Valentina;Deplano, Alberto

2026-01-01

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Abstract

For several decades, chalcone derivatives have been widely investigated for their extensive biological properties, owing to their versatile chemical scaffold and potent biological activity. Their relatively simple structure allows for diverse chemical modifications, improving pharmacological activities and selectivity. Chalcones have demonstrated great anticancer activity both in vitro and in vivo through different mechanisms, such as cell cycle arrest, microtubule destabilization, and apoptosis induction. These multiple mechanisms of action make chalcones particularly attractive as lead compounds in anticancer drug discovery. Researchers have also manipulated the chalcone scaffold to develop multitarget compounds that can simultaneously interact with different pathways, enhancing their activity and decreasing the emergence of drug resistance. This approach is particularly important in cancer treatment, given the involvement of different biological mechanisms in its development, allowing researchers to overcome the limitations of monotherapies.