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
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.