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review · Molecules

Indole Derivatives: A Versatile Scaffold in Modern Drug Discovery—An Updated Review on Their Multifaceted Therapeutic Applications (2020–2024)

202461 citationsOpen accessMinia University

In plain language

Indole derivatives serve as versatile chemical scaffolds in medicinal chemistry with broad biological activities. Recent progress over a five-year period shows these compounds playing active roles across multiple therapeutic areas, including cancer therapy, infectious disease control, anti-inflammatory interventions, neurodegenerative disease management, and metabolic disorder treatments. These molecular structures target a variety of biological pathways to support the creation of new therapeutic candidates. In particular, indole-based molecules display efficacy against drug-resistant pathogens and drug-resistant cancer cell lines. Furthermore, they provide prospective therapeutic routes for managing chronic conditions such as hypertension and diabetes. By addressing complex mechanisms across these diverse biological systems, indole scaffolds offer adaptable foundations for developing therapeutic agents aimed at persistent and difficult-to-treat health conditions.

Key takeaways

  • Indole derivatives demonstrate biological activity across oncology, infectious diseases, inflammation, neurodegeneration, and metabolic disorders.
  • The compounds effectively target drug-resistant cancer cells and resistant pathogens.
  • Indole-based scaffolds offer potential therapeutic avenues for managing chronic diseases including diabetes and hypertension.

Why it matters

Developing new therapies is vital as diseases become resistant to existing medications and chronic illnesses rise globally. Chemical scaffolds based on indole provide flexible building blocks capable of interacting with multiple disease pathways. Their activity against drug-resistant cancers and infections, alongside applications in conditions like diabetes, makes them significant assets for advancing treatments against urgent global health challenges.

Commercialisation angle

These findings are directly relevant to pharmaceutical companies and medicinal chemists seeking early-stage drug candidates for oncology, antimicrobial resistance, and chronic disease management. Because the work focuses on reviewing chemical scaffolds and laboratory-level biological mechanisms, the technology sits at an early discovery stage, remaining years away from real-world clinical use and commercial deployment.

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Abstract

Indole derivatives have become an important class of compounds in medicinal chemistry, recognized for their wide-ranging biological activities and therapeutic potential. This review provides a comprehensive overview of recent advances in the evaluation of indole-based compounds in the last five years, highlighting their roles in cancer treatment, infectious disease management, anti-inflammatory therapies, metabolic disorder interventions, and neurodegenerative disease management. Indole derivatives have shown significant efficacy in targeting diverse biological pathways, making them valuable scaffolds in designing new drugs. Notably, these compounds have demonstrated the ability to combat drug-resistant cancer cells and pathogens, a significant breakthrough in the field, and offer promising therapeutic options for chronic diseases such as diabetes and hypertension. By summarizing recent key findings and exploring the underlying biological mechanisms, this review underscores the potential of indole derivatives in addressing major healthcare challenges, thereby instilling hope and optimism in the field of modern medicine.

Research topics

  • Synthesis and Biological Evaluation
  • Click Chemistry and Applications
  • Synthesis and biological activity

Sustainable Development Goals

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DOI: 10.3390/molecules29194770

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