The chalcone has a central core for a variety of important biological activities and is composed of an aromatic ketone and an enone. Derivatives with the chalcone skeleton have been isolated from flowering plant species all over the the world. Some of these derivatives have significant biological properties such as anti-cancer, estrogenic, and anti-asthmatic. Analogs of chalcones are being studied to modify its biological properties and expand its therapeutic scope. These studies have proven that these analogs have cytotoxicity against several cancer cell lines. Our lab is focusing on the C-benzylated chalcone and its analogs to further tune them for specific biological properties. We have successfully developed a route to synthesize the C-benzylated chalcone from commercially available phloroglucinol. Currently, we are working on synthesizing different analogs of the C-benzylated chalcone by modifying the functionalities on the aromatic systems. To be presented is the synthetic route accessing the C-benzylated chalcone core structure, analogs, drug conjugates and <i>in vitro</i> biological assessment.

Efforts in the development of new anticancer therapies: C-benzylated chalcones and derivatives

253rd National Meeting (2017)

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