Dadashpour Sakineh, Emami Saeed
Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Eur J Med Chem. 2018 Apr 25;150:9-29. doi: 10.1016/j.ejmech.2018.02.065. Epub 2018 Feb 24.
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.
吲哚骨架是天然存在的和合成的生物活性化合物（包括抗癌剂）中最广泛存在的杂环之一。由于其生物多样性和多功能性，它一直是基于靶点设计和开发抗癌剂的高度优先基序。在过去十年中，许多研究人员报道了各种基于吲哚的化合物，它们具有产生潜在抗癌活性的不同机制，这表明吲哚基序在抗癌药物开发中的重要性。本文旨在综述吲哚核心在设计可能通过组蛋白脱乙酰酶（HDACs）、沉默调节蛋白、PIM激酶、DNA拓扑异构酶和σ受体等各种靶点发挥作用的新型抗癌剂中的当前应用。通过吲哚衍生化合物靶向癌细胞中的这些酶或受体可能是治疗癌症的有力工具。
