Chapter 3 - Privileged chalcone scaffolds in drug discovery

Abstract

Chalcones are typically privileged scaffolds found in many naturally occurring compounds. They are widely used as lead compounds for designing novel bioactive molecules with a series of potential pharmacologic activities. This review highlights evidence of chalcone as a privileged scaffold in medicinal chemistry as an update of our comprehensive review (Chem. Rev.2017; 117, 7762–7810). The simple chalcones according to Michael acceptor-related mechanisms (e.g., IκB kinases, thioredoxin reductase, and the Kelch-like ECH-associated protein 1–nuclear factor erythroid 2-related factor 2–antioxidant response element pathway) are principally classified. Representative hybrid chalcones are emphasized, including fused hybrid chalcones and linked hybrid chalcones. Moreover, future challenges and perspectives are provided to facilitate the development of chalcone derivatives in the medicinal chemistry community.