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Ind recent years, the indole core has emerged as a highly favored scaffold in drug research. Although indole was first shown to be an anticancer agent in vinca alkaloids, it also continued to exhibit many activities with various mechanisms in other diseases, such as diabetes, HIV, Alzheimer's, and hyperlipidemia. Indole derivatives have proved that they deserve researchers’ attention due to their biochemical diversity in plenty of plants, bacteria, animals, marine organisms, and humans, as well as the fact that they are used to synthesize several FDA-approved drugs. The main review’s objective is to compile a comprehensive listing of almost all reported pharmacological activities from 2011 to 2025, with the structure-activity relationship of potentially active compounds. It also highlights several green approaches and recent indole and indole derivative synthesis trends.
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