Chalcones and Their Synthetic Analogs

Chalcones is a collective name of natural and synthetic compounds with a 1,3-diaryl-2-propen-1-one moiety. Natural chalcones are biogenetic precursors of the flavonoids in higher plants. They belong to one of the major classes of naturally occurring compounds with widespread distribution in different plant families. Natural and synthetic chalcones display a wide variety of pharmacological effects, including antibacterial, antiprotozoal, antimalarial, anti-inflammatory activities, cytotoxicity towards cancer cell-lines, antitumor, and antitumor-promoting, activities. The chalcone scaffold is one of the natural privileged structures, which possess geometry suitable for decoration with side chains, such that the resulting products bind to different target proteins. The present contribution summarizes up-to-date summary of their synthetic methods, UV, IR and MS characterization, covalent and noncovalent interactions under cellular conditions, as well as antimalarial and anti-inflammatory actions of natural and synthetic derivatives. Synthesis and spectroscopic properties of not only chalcones but their conformationally restricted analogs are also discussed. Furthermore, synthetic methods and biological activities of C5-curcuminoids, a class of compounds with the related 3-aryl-2-propen-1-one moiety, are summarized. The respective chapters discuss the known structure-to-spectroscopic characteristic and structure-to-biological activity relationships as well.