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

Abstract

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 mole-cule inhibitors containing pyrazolo[1,5-a]pyrimidine scaffold and their structure-activity relation-ships are summarized and discussed to provide more reference value for the application of this par-ticular structure in antitumor drugs.