Recent Development in Indole Derivatives as Anticancer Agent: A Mechanistic Approach

Author(s): Neha Devi, Kamalpreet Kaur, Avadh Biharee, Vikas Jaitak*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 21 , Issue 14 , 2021

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Graphical Abstract:


Background: Cancer accounts for several deaths each year. There are multiple FDA approved drugs for cancer treatments. Due to the severe side effects and multiple drug resistance, the current drug therapies become ineffective. So, the newer moieties with fewer toxic effects are necessary for the development.

Objective: The mechanism of indole derivatives as anti-cancer agents with their major target is explored in detail in this article.

Methods: Recent advances and mechanism of indole derivatives as anti-cancer agents are reviewed. This review suggests a detailed explanation of multiple mechanisms of action of various indole derivatives: cell cycle arrest, aromatase inhibitor estrogen receptor regulator, tubulin inhibitor, a tyrosine kinase inhibitor, topoisomerase inhibitors, and NFkB/PI3/Akt/mTOR pathway inhibitors, through which these derivatives have shown promising anti-cancer potential.

Results: A full literature review showed that the indole derivatives are associated with the properties of inducing apoptosis, aromatase inhibition, regulation of estrogen receptor and inhibition of tyrosine kinase, tubulin assembly, NFkB/PI3/Akt/mTOR pathway, and HDACs. These derivatives have shown significant activity against cancer cell lines.

Conclusion: Indole derivatives seem to be important in cancer via acting through various mechanisms. This review has shown that the indole derivatives can further be explored for the betterment of cancer treatment, and to discover the hidden potential of indole derivatives.

Keywords: Indole, anti-cancer, cell cycle arrest, aromatase, estrogen, tubulin, tyrosine kinase, topoisomerase.

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Article Details

Year: 2021
Published on: 04 January, 2021
Page: [1802 - 1824]
Pages: 23
DOI: 10.2174/1871520621999210104192644
Price: $65

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