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Pyrazolo[1,5-a]pyrimidine Based Trk Inhibitors: Design, Synthesis, Biological Activity Evaluation
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-11-25 , DOI: 10.1016/j.bmcl.2020.127712 Yongjie Zhang 1 , Yan Liu 1 , Ying Zhou 1 , Qing Zhang 1 , Tianfu Han 1 , Chunlei Tang 1 , Weizheng Fan 1
中文翻译：
吡唑并[1,5-a]嘧啶类Trk抑制剂：设计，合成，生物活性评估
更新日期：2020-11-26
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-11-25 , DOI: 10.1016/j.bmcl.2020.127712 Yongjie Zhang 1 , Yan Liu 1 , Ying Zhou 1 , Qing Zhang 1 , Tianfu Han 1 , Chunlei Tang 1 , Weizheng Fan 1
Affiliation
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Tropomyosin receptor kinases (Trks), a transmembrane receptor tyrosine kinases, have attracted more and more attention as a drug target. Here we reported the structure-based synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidine derivatives as Trk inhibitors, which exhibited potent Trk inhibitory activities. Particularly, compounds 8a, 8f, 9a, 9b and 9f (IC50<5 nM) showed significant inhibitory potency against Trk.
中文翻译：
吡唑并[1,5-a]嘧啶类Trk抑制剂：设计，合成，生物活性评估
Tropomyosin受体激酶（Trks）是一种跨膜受体酪氨酸激酶，作为药物靶标已引起越来越多的关注。在这里，我们报告了新型的吡唑并[1,5-a]嘧啶衍生物作为Trk抑制剂的结构化合成和生物学评估，该化合物具有强大的Trk抑制活性。特别地，化合物8a，8f，9a，9b和9f（IC 50 <5nM）显示出对Trk的显着抑制效力。
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