咪唑吡啶基激酶抑制剂作为潜在抗癌药物的研究综述。
Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review.
发表日期：2023 Sep 03
作者：
Fariba Peytam, Zahra Emamgholipour, Alireza Mousavi, Mahfam Moradi, Roham Foroumadi, Loghman Firoozpour, Fatemeh Divsalar, Maliheh Safavi, Alireza Foroumadi
来源：
BIOORGANIC CHEMISTRY
摘要：
鉴于蛋白激酶在关键细胞过程中蛋白质磷酸化机制中的基础作用，尤其是在癌症中的失调，突显了它们的治疗相关性。咪唑吡啶是丰富的生物活性化合物中发现的多用途支架。鉴于其结构特征，咪唑吡啶具备与不同蛋白激酶相互作用的关键活性。这种特性激发了研究人员进行大量结构变化。在这篇综述中，我们包括对基于咪唑吡啶的小分子设计和生物评估的广泛调查，以探索其作为针对多种激酶的抗癌药物的潜在作用。我们描述了影响抑制能力的结构要素，阐明了它们的关键结构-活性关系 (SAR) 和作用方式（如有）。我们将这些化合物分为两组：丝氨酸/苏氨酸和酪氨酸抑制剂。通过强调咪唑吡啶在激酶抑制中的有前途的作用，我们旨在促进更加有效的定向化合物的设计和开发，以用于癌症治疗。版权所有© 2023 Elsevier Inc. 保留所有权利。
Considering the fundamental role of protein kinases in the mechanism of protein phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has underscored their therapeutic relevance. Imidazopyridines represent versatile scaffolds found in abundant bioactive compounds. Given their structural features, imidazopyridines have possessed pivotal potency to interact with different protein kinases, inspiring researchers to carry out numerous structural variations. In this comprehensive review, we encompass an extensive survey of the design and biological evaluations of imidazopyridine-based small molecules as potential agents targeting diverse kinases for anticancer applications. We describe the structural elements critical to inhibitory potency, elucidating their key structure-activity relationships (SAR) and mode of actions, where available. We classify these compounds into two groups: Serine/threonine and Tyrosine inhibitors. By highlighting the promising role of imidazopyridines in kinase inhibition, we aim to facilitate the design and development of more effective, targeted compounds for cancer treatment.Copyright © 2023 Elsevier Inc. All rights reserved.