Indole moiety is a magnificent nucleus in the development of anticancer drugs. The pharmacological profile of indole is excellent in targeting a wide range of proteins, enzymes. An indole has a nitrogen atom that is capable of forming hydrogen bonds with the targets emphasizing its potential. Many studies have demonstrated the effectiveness of indole in the treatment of cancer by working through various pathways. Indole-based drugs got market approval to be used as chemotherapeutics, such as vincristine and vinblastine which encourage researchers to work on indole derivatives for cancer treatment with a better pharmacokinetic profile. This prompted us to review on indole derivatives as anticancer agents to bring out their potential derivatives under study. This study encompasses literature published between 2014 and 2021 on indole scaffold that exhibits in vitro and in vivo potential against cancer by searching PubMed, Google Scholar, and Science Direct databases. The search terms were "anticancer", "indole", "cell lines", "structure-activity relationship" and "cytotoxic activity."[a] A.
Heterocyclic compounds are a class of compounds that is deeply intertwined with biological processes and are found in about 90% of commercially available medicines. They serve a critical function in medicinal chemistry and focused in the field of medication development for its intensive research due to their broad variety of biological effects because of their intriguing molecular architecture, indoles are good candidates for drug development. It is a bicyclic structure consisting of a six-membered benzene ring fused to a five-membered pyrrole ring with several pharmacophores that yield a library of different lead compounds. Human cancer cells have been demonstrated to be inhibited by indoles in the development of new anticancer medicines. This is the first comprehensive review to focus on current methodologies for incorporating indole moiety, with their mechanistic targets as anticancer drug, in order to shed light on the logical development of indole based anticancer treatment options with high efficacy. This compiled data may serve as a benchmark for modifying existing ligands in order to design novel potent molecules through excellent yield synthesis techniques.
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