Indenopyrazole as a Privileged Structure in the Development of Anticancer Agents
Indenopyrazole as a Privileged Structure in the Development of Anticancer Agents
复制标题
茚并吡唑作为抗癌药物开发中的优先结构
DOI：
10.12970/2308-8044.2017.05.01
复制
发表时间：
2017-01
期刊：
影响因子：
--
通讯作者：
Zhao-Peng Liu
中科院分区：
文献类型：
--
作者：
Ying-Jie Cui;Zhao-Peng Liu
双功能结构是一种分子支架，通过功能基团的修饰，可以为一系列不同的生物靶点提供有效的和选择性的配体。茚并吡唑是由苯环、中心5元环和吡唑环组成的三环杂环结构。茚并吡唑作为一种特殊的结构，近年来被广泛应用于多靶点抗癌药物的设计。许多茚并吡唑衍生物显示出有效的抗癌活性，如检查点激酶1、表皮生长因子受体、血管内皮生长因子、血小板衍生生长因子受体、细胞周期蛋白依赖性激酶和微管蛋白聚合抑制剂等。本文综述了茚并吡唑类化合物作为抗癌药物的研究进展，并讨论了它们的SAR。保留字：检查点激酶1，细胞周期蛋白依赖性激酶，表皮生长因子受体，缺氧诱导因子1，茚并吡唑，抑制剂，血小板衍生生长因子受体，特权结构，微管蛋白聚合，血管内皮生长因子。
A Privileged structureis a molecular scaffold that can provide potent and selective ligands for a range of different biological targets through modification of functional groups. Indenopyrazole is a three ringed heterocyclic structure consisting of a benzene ring, a central 5-membered ring and a pyrazole ring. As a privileged structure, indenopyrazole has been extensively used in recent years in the design of anticancer agents with versatile targets. A number of indenopyrazole derivatives displayed potent anticancer activities as checkpoint kinase 1, epidermal growth factor receptor, vascular endothelial growth factor, platelet-derived growth factor receptor, cyclin-dependent kinases, and tubulin polymerization inhibitors, among many others. This review will summarize the recent development of indenopyrazoles as anticancer agents, discuss their SARs. Keywords: Checkpoint kinase 1, cyclin-dependent kinases, epidermal growth factor receptor, hypoxia-inducible factor 1, indenopyrazoles, inhibitors, platelet-derived growth factor receptor, privileged structures, tubulin polymerization, vascular endothelial growth factor.