Pyrazolo[1,5-a]pyrimidines are fused heterocycles that have spawned many biologically active antitumor drugs and are important privileged structures for drug development. Pyrazolo[1,5- a]pyrimidine derivatives have played an important role in the development of antitumor agents due to their structural diversity and good kinase inhibitory activity. In addition to their applications in traditional drug targets such as B-Raf, KDR, Lck, and Src kinase, some small molecule drugs with excellent activity against other kinases (Aurora, Trk, PI3K-γ, FLT-3, C-Met kinases, STING, TRPC) have emerged in recent years. Therefore, based on these antitumor drug targets, small molecule inhibitors containing pyrazolo[1,5-a]pyrimidine scaffold and their structure-activity relationships are summarized and discussed to provide more reference value for the application of this particular structure in antitumor drugs.

中文翻译：

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吡唑并[1,5-a]嘧啶作为抗肿瘤药物支架的应用和SAR。

吡唑并[1,5-a]嘧啶是稠合杂环，产生了许多具有生物活性的抗肿瘤药物，并且是药物开发的重要特权结构。吡唑并[1,5-a]嘧啶衍生物由于其结构多样性和良好的激酶抑制活性，在抗肿瘤药物的开发中发挥了重要作用。除了应用于B-Raf、KDR、Lck、Src激酶等传统药物靶点外，一些针对其他激酶（Aurora、Trk、PI3K-γ、FLT-3、C-Met激酶）具有优异活性的小分子药物、STING、TRPC）是近年来兴起的。因此，基于这些抗肿瘤药物靶点，对含有吡唑并[1,5-a]嘧啶支架的小分子抑制剂及其构效关系进行总结和讨论，以期为这种特殊结构在抗肿瘤药物中的应用提供更多的参考价值。