Cancer has eventually stepped into the molecular insights focussing on the development of new generation of anticancer drugs especially of natural origin and its analogues with less or no toxicity issues and targeting specific molecular signalling pathways. In various therapeutic areas, numerous natural products and their derivatives have been effectively used to treat many human diseases or disorders. Chalcones, as metabolic precursors of some flavonoids and isoflavonoids have a structure of open chain flavonoids (1,3-diaryl-2-propen-1-ones) present in fruits and vegetables, possessing a broad range of biological activities including cancer chemotherapeutic and chemopreventive property. The anticancer properties of chalcones have been improved by substituting aryl rings (e.g. methoxy substitution on both aryl rings A and B) and introducing heterocyclic moieties. Hybridization with other pharmacologically important moieties (benzodiazepines, benzothiazoles, imidazolones etc.) by taking the help of SAR (structure-activity relationship) studies with much ease in preparation and oral administration ultimately has made chalcone a safe therapeutic agent. Some clinical trials revealed that these compounds did not cause toxicity and are present in plasma at optimum concentrations. Nowaday’s several chalcones are also used in cosmetic formulations and in food additives which could further be utilized for its chemopreventive potential. This book chapter briefly summarizes the demanding efforts made in the development of novel anticancer chalcones recorded in recent literatures with focussed cancer targets as well as presents an outline of the patents published in recent decades.
Keywords: Angiogenesis, antiproliferative, apoptosis, cancer, cell cycle arrest, cell line, chalcone, chalcone derivatives, chemoprevention, cytotoxicity, heterocyclic chalcone derivatives, IC50, metastasis, NFκB, p53, p21, p23, TRIAL, tumor.