4.5 Article

Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127712

关键词

Tropomyosin receptor kinases; Anticancer; Design and synthesis; Molecular docking

资金

  1. National First-class Discipline Program of Food Science and Technology [JUFSTR20180101]
  2. National Natural Science Foundation of China [21305051]

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Novel pyrazolo[1,5-a]pyrimidine derivatives were synthesized as Trk inhibitors, showing potent inhibitory activities against Trk. Particularly, compounds 8a, 8f, 9a, 9b, and 9f exhibited significant inhibitory potency against Trk with IC50 values < 5 nM.
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.

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