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Isatin (1H-indole-2,3-dione) and indole are versatile scaffolds with diverse pharmacological activities, including antimicrobial, anticancer, antiviral, anticonvulsant, anti-inflammatory, and analgesic effects. Isatin-indole hybrids have emerged as multifunctional agents with significant potential in drug discovery.
A literature survey (2010-2025) across major databases (PubMed, Google Scholar, ACS, etc.) included reports on synthesis, biological evaluation, and structure–activity relationship (SAR) analysis.
Numerous synthetic approaches, including both conventional and green methods, have yielded a diverse range of isatin-indole derivatives. Many exhibited potent antimicrobial, anticancer, antioxidant, and antitubercular activities, with SAR studies highlighting the impact of substitution patterns on activity and selectivity.
This review aims to provide a comprehensive overview of hybrid molecules in which the isatin core is covalently linked to an indole scaffold. It focuses on their synthesis, diverse biological activities and structure-activity relationship (SAR) studies from 2001 onwards.
This review provides a concise summary of the latest developments and future outlook for the therapeutic potential of isatin-indole hybrids in the development of potent bioactive drugs.
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