Application and SARs of Pyrazolo[1,5-a]pyrimidine as Antitumor Agents Scaffold.

IF 2.9 4区医学 Q3 CHEMISTRY, MEDICINAL

Current topics in medicinal chemistry Pub Date : 2023-01-01 DOI:10.2174/1568026623666230228111629

Yadong Zhang, Di Wen, Jiwei Shen, Lu Tian, Yan Zhu, Jifang Zhang, Leyan Zhao, Shi Ding, Ju Liu, Ye Chen

引用次数: 0

Abstract

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.

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吡唑[1,5-a]嘧啶作为抗肿瘤药物支架的应用及反应反应。

Pyrazolo[1,5-a]嘧啶是一种融合的杂环化合物，已经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。吡唑啉[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。除了在传统药物靶点如B-Raf、KDR、Lck和Src激酶上的应用外，近年来出现了一些对其他激酶(Aurora、Trk、PI3K-γ、FLT-3、C-Met激酶、STING、TRPC)具有优异活性的小分子药物。因此，基于这些抗肿瘤药物靶点，对含吡唑[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探讨，为该特定结构在抗肿瘤药物中的应用提供更多参考价值。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current topics in medicinal chemistry 医学-医药化学

CiteScore

6.40

自引率

2.90%

发文量

186

审稿时长

3-8 weeks

期刊介绍： Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.