Application and SARs of pyrazolo[1,5-a]pyrimidine as antitumor agents scaffold.

doi:10.2174/1568026623666230228111629

Paper

Application and SARs of pyrazolo[1,5-a]pyrimidine as antitumor agents scaffold.

Published Feb 28, 2023 · Yadong Zhang, Di Wen, Jiwei Shen

Current topics in medicinal chemistry

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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.

Study Snapshot

Pyrazolo[1,5-a]pyrimidines are important structures for antitumor drug development due to their structural diversity and kinase inhibitory activity against various kinases.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Application and SARs of pyrazolo[1,5-a]pyrimidine as antitumor agents scaffold.

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