Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation

Yiqing Fan,Yongjie Zhang, Yan Liu,Hongyu Jiang,Ying Zhou,Chunlei Tang,Weizheng Fan

Bioorganic & Medicinal Chemistry Letters（2022）

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摘要

•New pyrido[1,2-α]pyrazole derivatives were designed and synthesized.•Wild-type TrkA, TrkAG595R and Alk inhibitory activity in vitro were evaluated.•Compound 14h and 14j behaved as excellent Second-generation inhibitor against Trk, and 14j was a selective inhibitor for Trk.

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关键词

Tropomyosin receptor kinase,The next-generation Trk inhibitor,Antitumor,Design and synthesis,High selectivity

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