Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

Dhiman, A M; Sharma, Rupam; Singh, Rajesh

doi:10.1016/j.apsb.2022.03.021

Cited by 84 publications

(43 citation statements)

References 127 publications

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“…Its derivatives possess a broad spectrum of biological activities, including antimicrobial [ 12 , 13 , 14 , 15 ], antitubercular [ 16 , 17 , 18 ], anti-tumor [ 19 , 20 , 21 , 22 , 23 ], antiviral [ 17 , 24 , 25 ], antioxidant [ 12 , 21 ], anti-inflammatory [ 17 , 25 , 26 , 27 ], antifungal [ 28 , 29 , 30 ], antimalarial [ 17 , 31 ], antidepressants [ 17 ], antidiabetic [ 25 , 26 , 32 ], аnti-Alzheimer’s [ 26 , 33 ], and antibacterial [ 26 , 34 ] properties.…”

Section: Introductionmentioning

confidence: 99%

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

2023

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Indoles and hydantoins are important heterocycles scaffolds which present in numerous bioactive compounds which possess various biological activities. Moreover, they are essential building blocks in organic synthesis, particularly for the preparation of important hybrid molecules. The series of hybrid compounds containing indoles and imidazolidin-2-one moiety with direct С─С bond were synthesized using an amidoalkylation one-pot reaction. All compounds were investigated as a growth regulator for germination, growth and development of wheat seeds (Triticum aestivum L). Their effect on drought resistance at very low concentrations (4 × 10−5 М) was evaluated. The study highlighted identified the leading compounds, 3a and 3e, with higher growth-regulating activity than the indole-auxin analogues.

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Section: Introductionmentioning

confidence: 99%

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

2023

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“…These analogous molecules of 3-acyl indoles are very important molecules as they play a significant role in anticancer therapy …”

Section: Resultsmentioning

confidence: 99%

DDQ/Fe(NO₃)₃-Catalyzed Aerobic Synthesis of 3-Acyl Indoles and an In Silico Study for the Binding Affinity of N-Tosyl-3-acyl Indoles toward RdRp against SARS-CoV-2

et al. 2023

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In the present study, we herein report a DDQ-catalyzed new protocol for the synthesis of substituted 3-acylindoles. Being a potential system for virtual hydrogen storage, introduction of catalytic DDQ in combination with Fe(NO3)3·9H2O and molecular oxygen as co-catalysts offers a regioselective oxo-functionalization of C-3 alkyl-/aryllidine indolines even with scale-up investigations. Intermediate isolation, their spectroscopic characterization, and the density functional theory calculations indicate that the method involves dehydrogenative allylic hydroxylation and 1,3-functional group isomerization/aromatization followed by terminal oxidation to afford 3-acylindoles quantitatively with very high regioselectivity. This method is very general for a large number of substrates with varieties of functional groups tolerance emerging high-yield outcome. Moreover, molecular docking studies were performed for some selected ligands with an RNA-dependent RNA polymerase complex (RdRp complex) of SARS-CoV-2 to illustrate the binding potential of those ligands. The docking results revealed that few of the ligands possess the potential to inhibit the RdRp of SARS-Cov-2 with binding energies (−6.7 to −8.19 kcal/mol), which are comparably higher with respect to the reported binding energies of the conventional re-purposed drugs such as Remdesivir, Ribavirin, and so forth (−4 to −7 kcal/mol).

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“…Indole consists of a benzene ring fused at the 2-position and 3-position of the pyrrole ring. Its derivatives exert antitumor activity as inhibitors of tubulin polymerization and topoisomerase and as inducers of apoptosis, aromatase, and kinase inhibitors [ 75 ]. Indole derivatives with anti-melanoma activity are presented in Figure 7 .…”

Section: The Most Potent Anti-melanoma Agent From Most Recent Studies...mentioning

confidence: 99%

New Potential Agents for Malignant Melanoma Treatment—Most Recent Studies 2020–2022

Kozyra

Krasowska

Pitucha

2022

IJMS

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Malignant melanoma (MM) is the most lethal skin cancer. Despite a 4% reduction in mortality over the past few years, an increasing number of new diagnosed cases appear each year. Long-term therapy and the development of resistance to the drugs used drive the search for more and more new agents with anti-melanoma activity. This review focuses on the most recent synthesized anti-melanoma agents from 2020–2022. For selected agents, apart from the analysis of biological activity, the structure–activity relationship (SAR) is also discussed. To the best of our knowledge, the following literature review delivers the latest achievements in the field of new anti-melanoma agents.

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Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

Cited by 84 publications

References 127 publications

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

DDQ/Fe(NO₃)₃-Catalyzed Aerobic Synthesis of 3-Acyl Indoles and an In Silico Study for the Binding Affinity of N-Tosyl-3-acyl Indoles toward RdRp against SARS-CoV-2

New Potential Agents for Malignant Melanoma Treatment—Most Recent Studies 2020–2022

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Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

Cited by 84 publications

References 127 publications

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

DDQ/Fe(NO3)3-Catalyzed Aerobic Synthesis of 3-Acyl Indoles and an In Silico Study for the Binding Affinity of N-Tosyl-3-acyl Indoles toward RdRp against SARS-CoV-2

New Potential Agents for Malignant Melanoma Treatment—Most Recent Studies 2020–2022

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DDQ/Fe(NO₃)₃-Catalyzed Aerobic Synthesis of 3-Acyl Indoles and an In Silico Study for the Binding Affinity of N-Tosyl-3-acyl Indoles toward RdRp against SARS-CoV-2