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Abstract Background Various bioactive aromatic compounds containing the indole nucleus showed clinical and biological applications. Indole scaffold has been found in many of the important synthetic drug molecules which gave a valuable idea for treatment and binds with high affinity to the multiple receptors helpful in developing new useful derivatives. Main text Indole derivatives possess various biological activities, i.e., antiviral, anti-inflammatory, anticancer, anti-HIV, antioxidant, antimicrobial, antitubercular, antidiabetic, antimalarial, anticholinesterase activities, etc. which created interest among researchers to synthesize a variety of indole derivatives. Conclusion From the literature, it is revealed that indole derivatives have diverse biological activities and also have an immeasurable potential to be explored for newer therapeutic possibilities.