Chalcones are a group of naturally occurring compounds that have biological effects that include anti-inflammatory, anti-cancer, and antibacterial properties. Current chalcone research, including their synthesis, structure–activity relationships, and biological activities, is summarized herein. Along with their toxicity and safety profiles, the prospective usage of chalcones in medicinal research and development is discussed. This review emphasizes the need for additional research in order to fully examine the therapeutic potential of chalcones as therapeutic agents for the treatment of a variety of disorders.