A simple structure found in naturally occurring compounds, chalcone has been utilised in medicinal chemistry to generate drugs that show promise in treating a range of illnesses. Here, we discuss the synthesis, properties, and structural diversity of chalcones. We next go over how chalcones are made and their biological properties, including their antibacterial, anti-inflammatory, anti-cancer, and antioxidant properties, highlighting the relationships between structure and activity. Chalcone derivatives continue to enthral medical scientists due to their straightforward synthesis, straightforward chemistry, ease of working with hydrogen atoms, and a number of intriguing biological functions. Chalcones have not yet gotten the recognition they merit despite their enormous potential as chemical feedstock for the creation and development of new, potent drugs.