Natural products have played an evergreen role in the discovery of novel drugs to treat various human diseases since ancient times. Further, the potential therapeutic outcomes of natural scaffolds continue in modern drug discovery with the application of medicinal chemistry approaches. For example, polyphenols are the principal secondary metabolites that have attracted considerable attention due to their pharmacological actions as well as their nutritional and health-promoting benefits. Particularly, flavonoids are the greatest natural oxyheterocycles that exist in various dietary sources and play a strategic role against the cellular oxidation pattern, which is very important in the prevention of various metabolic diseases such as diabetes, cancer, obesity, and neurological disorders. In this context, chalcones, dihydrochalcones, flavanones, and aurones are pronounced as minor flavonoids that are useful as templates for the development of new drug candidates as well as for materials science applications. Considering the prominence of natural compounds, this study aimed to discuss the importance of minor flavonoids and their recent advances, as described in the following sections.