Indole as a biological scaffold: a comprehensive review
Abstract
3-amino indole derivatives are a significant class of heterocyclic compounds in organic synthesis, known for their diverse applications in medicinal chemistry. Recent advancements in their synthesis have led to methods that enhance yield and efficiency, making these derivatives more accessible for research and pharmaceutical novel drug development. For decades, researchers have concentrated on generating indole heterocyclic molecules with novel biological and pharmacological features based on available and emerging information. Because of their beneficial bioactivities, we have discussed various bioactive indoles and their biological activities in this review paper.
Keywords:
Heterocylic compounds, novel drug development, bioactive indoles
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References
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2. N. A. Mukhtar, M. Suleiman, H. M. Al-Maqtari, K. T. Das, A. Bhat, J. Jamalis, "New Insights into the Modifi-cations and Bioactivities of Indole-3-Carboxaldehyde and its Derivatives as a Potential Scaffold for Drug Design: A Mini-Review.," Mini-Reviews in Medical Chemistry, 2025. https://doi.org/10.2174/0113895575351704241120060746
3. Z. Kazemi, H. Rudbari, N. Moini, F. Momenbeik, F. Carnamucio, N. Micale, "Indole-Containing Metal Complexes and Their Medicinal Applications," Molecules, 2024. https://doi.org/10.3390/molecules29020484
4. J. T. Kuethe, "A General Approach to Indoles: Prac-tical Applications for the Synthesis of Highly Functionalized Pharmacophores," Swiss Chemical So-ciety, 2006. https://doi.org/10.2533/chimia.2006.543
5. H. Sachdeva, J. Mathur, A. Guleria, "INDOLE DERIVA-TIVES AS POTENTIAL ANTICANCER AGENTS: A RE-VIEW," Sociedad Chilena de Qumica, 2020. https://doi.org/10.4067/s0717-97072020000204900
6. J. Dhuguru, R. Skouta, "Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents," Multidisciplinary Digital Publishing Institute, 2020. https://doi.org/10.3390/molecules25071615
7. E. Barresi et al., "Indole-Based Compounds in the Development of Anti-Neurodegenerative Agents," Molecules, 2024. https://doi.org/10.3390/molecules29092127
8. A. Singh et al., "A Mini-Review on the Synthesis of Pyrazinoindole: Recent Progress and Perspectives," Mini-Reviews in Organic Chemistry, 2020. https://doi.org/10.2174/1570193x17999200806151209
9. G. E. Bell, J. W. B. Fyfe, E. M. Israel, A. M. Z. Slawin, M. Campbell, A. J. B. Watson, "Synthesis of 2-BMIDA Indoles via Heteroannulation: Applications in Drug Scaffold and Natural Product Synthesis," American Chemical Society, 2022. https://doi.org/10.1021/acs.orglett.2c00959
10. V. Kasi et al., "Magnetic Nanoparticle-Catalysed One-Pot Multicomponent Reactions (MCRs): A Green Chemistry Approach," Catalysts, 2025. https://doi.org/10.3390/catal15090800
11. Sreelatha Kamera, Vishnu K. Sharma, Srivani M, Achaiah Garlapati, Design, Synthesis, Molecular Dock-ing, Antitubercular, Antimicrobial and Antioxidant Studies of Some Novel 3-(((1H-Benzo[d]imidazol-2-yl)methyl)thio)-5H-[1,2,4] Triazino[5,6-b]indole De-rivatives, International Journal of Pharmaceutical Sci-ences and Drug Research, 2023;15(4):494-506.
12. P. Muthumani, R. Meera, Suraj Bansal Agarwal, P. Devi, Synthesis of some derivatives of pyrimidine, oxadiazole and indole in combination by conventional and microwave method. Der Pharma Chemica; 2009, 1 (1): 167-17.
13. Jithila Rajan, Saranya Krishnan, Sruthi V Menon, Subin Mary Zachariah, In Silico Design, Synthesis, Characterization, In Vitro Anti-Inflammatory, and Antioxidant Studies of 4-Aryl-4h-Chromene Derivatives, Asian J Pharm Clin Res, Vol 10, Issue 7, 2017, 408-413
14. Esra Tatar, Sevgi Karakuş, Dharmarajan Sriram, Pe-rumal Yogeeswari, Design, Synthesis, and Molecular Docking Studies of a Conjugated Thiadiazole–Thiourea Scaffold as Antituberculosis Agents. Biol. Pharm. Bull. 2016, 39, 502–515.
15. Junjie Ma, Guanglong Bao, Limei Wang, Wanting Li, Design, synthesis, biological evaluation and prelimi-nary mechanism study of novel benzothiazole deriva-tives bearing indole-based moiety as potent antitu-mor agents, European Journal of Medicinal Chem-istry 96 (2015) 173-186.
16. Yuou Teng and Peng Yu. Design, synthesis and bio-logical activity evaluation of novel anticancer agent 5-(2-carboxyethenyl)indole derivatives, J. Chem. Pharm. Res., 2014, 6(9):376-380.
17. Rakesh jalandra, Gunjan Jadon, A Review Article on Indole, International Journal of Advanced Research in Pharmaceuticals & Biological sciences: 2014, 4(1),1-5.
18. Nehal A. Hamdy, Manal M. Anwar, Khadiga. Abu-Zied and Hanem M. Awad, Synthesis, Tumor In-hibitory and Antioxidant Activity of New Polyfunc-tionally 2-Substituted 5,6,7,8-Tetrahydronaphthalene Derivatives Containing Pyridine, Thioxopyridine and Pyrazolopyridine Moieties, Acta Poloniae Pharmaceutica and Drug Research, Vol. 70(6), pp. 987-1001, 2013.
19. Seetaramswamy S, Sekar V, Gandhimathi S, Laxmanadoss Murugesan, Perumal P, Synthesis and In-Vitro Anticancer Activity of Some Novel Bis -Benzothiazole Derivatives; International Journal Of Current Pharmaceutical Research, 5(2), 2013.
20. S.Biswal, U.Sahoo, S.Sethy, H.K.S Kumar, M.Banerjee, Indole: The Molecule of Diverse Biological Activities, Vol 5, Issue 1, 2012, 1-6.
21. Ankur Patel, D. Giles, Guru Basavarajaswamy , C. Sreedhar, Synthesis, pharmacological evaluation and molecular docking studies of indanone derivatives. Med Chem Res. Vol. 5, 2012, p-01-09
22. Hardik Patel, Nilesh Darji, Jagath Pillai and Bhagirath Patel, Recent Advance In Anti-Cancer Activity of In-dole Derivatives, Int. J. Drug Res. Tech. 2012, Vol. 2 (3), 225-230.
23. M. K. Oksal Akkoc et al. Design, synthesis, and biological evaluation of indole-based 1,4-disubstituted piperazines as cytotoxic agents, Turk J Chem 36 (2012), 515 – 525.
24. Srivastava, Anupam, Pandeya, S.N, Indole-A Versatile Nucleus in Pharmaceutical Field, International Journal of current Pharmaceutical review and Re-search, 1(3), 2011, 1-16.
25. Ekhlass, Nassar et. al. (2010), “Synthesis (in vitro) Antitumor and Antimicrobial Activity of some Pyra-zoline, Pyridine, and Pyrimidine Derivatives Linked to Indole Moiety”, Journal Of American Science, 6 (8), 463-471.
26. Lucia Kavacikova, Marta, Magdalena, Andrej, Milan. Development of Novel Indole-Based Bifunctional Al-dose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications. Molecules, 2021 May 12;26(10):2867. doi: 10.3390/molecules26102867.
Published
04/11/2025
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How to Cite
Seepana, S., V. Verma, P. Sharma, J. Sharma, and R. N. “Indole As a Biological Scaffold: A Comprehensive Review”. International Journal of Pharmacognosy and Chemistry, Vol. 6, no. 4, Nov. 2025, pp. 34-42, doi:10.46796/ijpc.v6i4.763.
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