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苯并五元杂环化合物抑制SHP2生物活性研究
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Abstract:
为拓展含苯并噻二唑结构单元的SHP抑制剂的化学空间，我们将苯并噻二唑结构单元转化为苯并噻唑、苯并咪唑、吲哚等结构单元，设计并合成了8个苯并五元杂环化合物。活性测试结果表明，部分化合物对SHP2显示了一定强度的抑制活性。其中化合物14 (IC50 = 26.22 μM)对SHP2显示了中等强度的抑制活性。
To explore the chemical space of SHP2 inhibitors by changing Benzo[c][1,2,5]thiadiazole moiety in-to Benzo[c]heterocycle moiety, a series of Benzo[c]heterocyclic compounds have been designed, synthesized and evaluated their biological activities against SHP2. Among them, compound 14 dis-played moderate inhibitory activity with IC50 of 26.22 μM against SHP2.
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