AbstractIn recent years, the incidence of cancer is high around the world, and the resistance of bacteria is increasing. To cope with the potentially adverse side effects of cancer chemotherapy and surgery, researchers are turning to the construction of new drug scaffolds. The indoline structure exists in a huge number of natural products, but drugs with indoline have only been formally studied in recent years. With the deepening of research, drugs containing indoline have played important roles in more disease treatment aspects, such as anti‐tumor, anti‐bacterial, anti‐inflammatory and have been used as analgesics, to treat cardiovascular diseases and so on. The synthesis and pharmacological activity of indoline derivatives is summarized in this review in order to support the addition of the indoline component to the toolbox of medicinal chemists. This review focuses on the advantages of indoline compounds in development and synthesis of and for the use as anticancer drugs, antibacterial drugs, to treat cardiovascular diseases and as anti‐inflammatory and analgesic drugs. Indoline structures are commonly found in natural and synthetic compounds with medicinal value and are now beginning to be exploited as the basic backbone of various drugs. As research continues, dihydroindoles and their derivatives will play a greater role in the medical field.