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Volume 21, Issue 18
  • ISSN: 1570-1808
  • E-ISSN: 1875-628X

Abstract

Isatin has garnered significant interest due to its wide range of pharmacological activities, including anti-inflammatory, anti-HIV, anticancer, antioxidant, antimicrobial, and antifungal properties. As a natural compound found in both humans (as a metabolic derivative of adrenaline) and plants (melastatin), its unique structure, with carbonyl groups at positions 2 and 3 and an NH group at position 1, makes it a valuable scaffold for designing bioactive analogs. Researchers have employed various strategies to enhance these analogs' pharmacological properties, with studies consistently highlighting their multitarget potential. This review focuses on isatin derivatives in medicinal chemistry, particularly as chemotherapeutic agents, and outlines common synthetic methods and recent advances in their biological and therapeutic applications. Notably, substitution at the C-5 position with electron-donating groups (EDGs) has shown strong antitumor activity against HepG2 cells (IC = 6.99 µM), approaching the efficacy of doxorubicin (IC = 3.56 µM). Modifications at the C-3 carbonyl group have also demonstrated 300-fold increased potency at 0.03 µM against Jurkat T lymphocytes. Structural variations within the isatin scaffold have shown significant cytotoxicity across several cancer cell lines, underscoring their potential in anticancer drug development.

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2024-11-29
2025-06-22

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/content/journals/lddd/10.2174/0115701808344031241126104914
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Advances in Isatin-derived Compounds for Modern Cancer Therapy: A Comprehensive Review
Letters in Drug Design & Discovery 21, 4134 (2024); https://doi.org/10.2174/0115701808344031241126104914
/content/journals/lddd/10.2174/0115701808344031241126104914
/content/journals/lddd/10.2174/0115701808344031241126104914
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  • Article Type:     Review Article
Keyword(s): 1H indole 2; 3-dione; adrenaline; Isatin; isatin derivatives; melosatin

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