苯并五元杂环化合物抑制SHP2生物活性研究  

Biological Evaluation of Benzo[c]heterocyclic Compounds against SHP2

作　　者：冯勃 陈晓禹 RajendranSatheeshkumar 王文龙 

机构地区：[1]江南大学药学院,江苏 无锡

出　　处：《药物化学》2020年第3期79-83,共5页Hans Journal of Medicinal Chemistry

摘　　要：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.

关 键 词：苯并五元杂环化合物 SHP2^PTP 抑制剂 构效关系 

分 类 号：O62[理学—有机化学]