Title:A Review on Indole as a Cardinal Scaffold for Anticancer Drugs Development
Volume: 20
Issue: 4
Author(s): Meenakshi Rana, Rajeev Ranjan, Niladry Sekhar Ghosh, Dharmendra Kumar*Ranjit Singh
Affiliation:
- Narayan Institute of Pharmacy, Gopal Narayan Singh University, Jamuhar,
Sasaram, Rohtas, Bihar, 821305, India
Keywords:
Cancer, indole derivatives, chemotherapy, drug development, novel anti-cancer molecules, anti-cancer drug resistance.
Abstract: Chemotherapy is the mainstay of therapeutic cancer therapy; however, the development of
resistance typically makes it less effective. There are continuous efforts by researchers to find novel
lead compounds with potent anti-cancer activity. Generally, synthetic or natural heterocyclic compounds
have been investigated in detail as a scaffold for cancer therapeutics. Among them, indole,
owing to its unique physiochemical and biological properties, provides a promising platform for the
development of pharmacophores for drug development against cancer, acting via various mechanisms.
Till now, several indole-based derivatives have been identified as anti-cancer agents, which
are either being used in clinics or are in various phases of clinical trials, suggesting their importance
in anti-cancer drug development. These anti-cancer drugs have been classified into different classes
depending on their mechanism of action. For example, histone deacetylase inhibitors (HDAC inhibitors),
silent mating type information regulation 2 homolog (SIRT) inhibitors, tubulin inhibitors,
proviral insertion site in Moloney murine leukemia virus (Pim) inhibitors, DNA Topoisomerase
inhibitors, and kinase inhibitors. In this review, the author's approach is to compile the recent
developments on indole-based anti-cancer drugs and provide insight into the respective structureactivity
relationships (SARs) of the compounds. We hope the review will provide a thorough understanding
to the reader and guide to developing novel and potent indole-based anticancer agents
against drug-sensitive and drug-resistant cancer in the future.