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.
