The indole scaffold is one of the most widespread heterocycles in the naturally occurring and synthetic bioactive compounds including anticancer agents. Due to its biodiversity and versatility, it has been a highly privileged motif for the target-based design and development of anticancer agents. In the last decade, many researchers have reported various indole-based compounds with distinct mechanisms involved in producing potential anticancer activities, indicating the importance of indole motif in the anticancer drug development. The present article aims to review the current application of indole core in the design of new anticancer agents that may act via various targets such as histone deacetylases (HDACs), sirtuins, PIM kinases, DNA topoisomerases and σ receptors. Targeting these enzymes or receptors in cancer cells by indole-derived compounds can be a powerful tool for the management of cancer.
Keywords: Anti-cancer; Cytotoxic activity; Drug design; Indole.
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