Indole Synthesis and Bioactivity Assessment
Summary
Indole and its derivatives constitute a foundational scaffold in both natural products and pharmaceutical chemistry, distinguished by a bicyclic system combining a benzene ring fused to a pyrrole moiety. Synthetic access to indoles has evolved from classical Fischer and Madelung protocols to modern approaches featuring selective C–H activation, cross-coupling and organocatalytic methods. Emphasis on sustainability has driven the adoption of metal-free and aqueous processes, organocatalysis and recyclable catalysts. Concurrently, the biological evaluation of indole frameworks spans anticancer, anti-inflammatory, antimicrobial and neuroprotective assays, with structure-activity relationships guided by cell-based screening, receptor-binding studies and membrane interaction analyses. Advances in modular assembly and late-stage functionalisation have enabled rapid diversification of indole libraries, accelerating the discovery of bioactive leads and facilitating translation into therapeutic candidates.
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Indole Synthesis and Bioactivity Assessment publication trend
The graph below shows the total number of articles in indole synthesis and bioactivity assessment across all publications each year (not limited to Nature Index journals).
Technical terms
Heterocycle: A ring structure containing at least one non-carbon atom such as nitrogen, oxygen or sulfur.
Diindolylmethanes (DIMs): Bis-indole compounds joined through a central methylene bridge, noted for anti-inflammatory and anti-cancer properties.
Mannich reaction: A three-component condensation involving an aldehyde, amine and activated C–H compound to form β-aminocarbonyl frameworks.
Electrophilic substitution: A reaction in which an electrophile selectively replaces a hydrogen atom on an aromatic system.
Decarboxylative coupling: A bond-forming process where carboxylate groups are removed as carbon dioxide to enable cross-coupling between substrates.
References
- Synthesis of Tumor Selective Indole and 8-Hydroxyquinoline Skeleton Containing Di-, or Triarylmethanes with Improved Cytotoxic Activity. Molecules (2024).
- Iodine-catalyzed electrophilic substitution of indoles: Synthesis of (un)symmetrical diindolylmethanes with a quaternary carbon center. Beilstein Journal of Organic Chemistry (2021).
- Decarboxylative Coupling Reaction of 2‐(1H‐Indol‐3‐yl)acetic Acids with Indole, Azaindole, Benzimidazole and Indazole Derivatives. Advanced Synthesis & Catalysis (2019).
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