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Screening, Synthesis and Biological Evaluation of Novel Bruton’s Tyrosine Kinase Inhibitors

  • Qiu-Ya Xu,
  • Rong-Chen Li,
  • Zhu Li,
  • Wen-Jiang Ma,
  • Yu-Ning Gao,
  • Hui-Yu Chen,
  • Zhen-Jiang Liu

摘要

Three potential BTK inhibitors were identified in a ZINC15 database by the virtual screening method. The three molecules were synthesized by reasonable synthetic routes to allow biological evaluation. Their antiproliferative activity was tested in vitro on the Ramos cell line. The results showed that 5-(((4,6-dimethylpyrimidin-2-yl)thio)methyl)-N-(1H-indol-4-yl)furan-2-carboxamide (Y7) had a moderate inhibitory effect on the proliferation of lymphoma Ramos cells with an IC50 value of 207.8 μM, which could provide important theoretical reference for the discovery of novel BTK inhibitors.