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.

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.…”

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.…”

Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies

“…Moreover, indole derivatives represent a significant source of novel antibacterial agents that may exhibit their biological activity through the inhibition of efflux pumps, biofilm or filamentous temperature-sensitive protein Z (FtsZ), and methicillin-resistant Staphylococcus aureus pyruvate kinase [17][18][19][20][21][22]. Particular attention has been paid to indole-containing compounds with anticancer properties, which exert their activity by affecting numerous biological targets [23][24][25]. For example, the tubulin inhibitors vincristine and vinblastine isolated from Catharanthus roseus are used in the treatment of various cancers [26], whereas dacomitinib is a well-known antitumor agent that blocks the activity of epidermal growth factor receptor (EGFR) [27].…”