Indole Derived Anticancer Agents

Abstract

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.

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

“…[43] Natural products, colours, medicines, organic materials, and notably pharmacologically promising compounds all include N-heterocycles. [4,44] These N-heterocyclic compounds such as triazine, [45] indole, [46] oxadiazole, [47] acridine, [48] benzimidazoles, [49] benzothiazoles, [50] imidazole, [51] isoxazole, [52] thiazolidine, [53] triazoles, [54] quinolines, [55] pyrimidine, [56] pyrazole [57] and quinazolines garnered a lot of interest in recent years due to their wide range of activities. [58] These N-heterocyclic described anticancer effects in numerous types of cancer through limiting cell growth, inducing cell differentiation and apoptosis.…”

Aqueous Extract of Dillenia indica Fruit (AEDI): A Sustainable Biocatalyst for the Synthesis of Pharmacologically Important Bis(indolyl)methanes

“…Many natural compounds and bioactive chemicals have indole frameworks. [23][24][25] Particularly intriguing are 7-bis(indolyl) methanes (BIMs), which are said to exhibit a wide range of biological functions (Figure 1). Examples include compound (I) which is cytotoxic to MCF-7 cells, [26] compound (II) which exhibits anticancer activity against human cervical cancer (HeLa) cells, [27] compound (III) which exhibits anti-fungal properties, [28] and compounds (IV) to (VI) which are isolated from bacterial broths and exhibit amazing alkaloid properties.…”

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

“…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.…”