基于吡咯并[2,3-d]嘧啶的激酶抑制剂已成为对抗各种类型癌症的一类重要的靶向治疗药物。吡咯并嘧啶环系统独特的结构特征为设计各种激酶的有效抑制剂提供了一个适应性强的平台，这对于调节细胞过程至关重要。吡咯并嘧啶固有的脱氮嘌呤框架与天然配体 ATP 腺嘌呤非常相似。结构模拟增强了它们作为关键激酶的有效抑制剂的吸引力。这篇综述探讨了设计和开发基于吡咯并嘧啶的衍生物的复杂过程，强调了它们的结构多样性以及用于增强选择性、效力和药代动力学特性的策略修饰。讨论深入探讨了药物化学策略，重点介绍了已进入临床评估的成功范例。此外，该综述强调了吡咯并嘧啶支架在彻底改变靶向癌症治疗方面的前景，并为未来方向提供了开创性的视角。版权所有 © 2024 Elsevier Inc. 保留所有权利。

Pyrrolo[2,3-d]pyrimidine-based kinase inhibitors have emerged as an important class of targeted therapeutics to combat various types of cancer. The distinctive structural feature of pyrrolopyrimidine ring system offers an adaptable platform for designing potent inhibitors of various kinases, crucial in regulating cellular processes. The deazapurine framework inherent to pyrrolopyrimidines bears a conspicuous resemblance to adenine, the natural ligand ATP. The structural mimicry enhances their appeal as potent inhibitors of key kinases. This review reconnoitres the intricate process of designing and developing pyrrolopyrimidine based derivatives, accentuating their structural diversity and the strategic modifications employed to enhance selectivity, potency, and pharmacokinetic properties. The discussion delves into medicinal chemistry strategies, highlighting successful examples that have been progressed to clinical evaluation. Furthermore, the review highlights the promise of pyrrolopyrimidine scaffolds in revolutionizing targeted cancer therapy and provides a pioneering perspective on future directions.Copyright © 2024 Elsevier Inc. All rights reserved.