Chalcones constitute a group of phenolic compounds that command an increasing
interest on cancer research. Natural chalcones are widespread through the plant kingdom. The most abundant
and investigated chalcones are isoliquiritigenin, flavokawain and xanthohumol, which are present in the Fabaceae,
Piperaceae, Cannabaceae, and Moraceae families. These chalcones have been shown to be promising
lead antitumor-chemopreventive drugs by three different activities: antioxidants, cytotoxic and apoptosis inducers.
In the recent years, SAR (structure-activity relationship) has contributed towards the improvement of
anticancer properties of chalcones by substituting aryl rings and introducing heterocyclic moieties. This review
summarizes the anticancer activities shown by natural chalcones and the SAR and describes how different
chemical moiety modifications could lead them to be therapeutically useful in the treatment of cancer.
Keywords: Apoptosis, cancer, chalcone, chemoprevention, flavonoid, synthesis, tubulin.
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