%0 Journal Article
%T 苯并五元杂环化合物抑制SHP2生物活性研究<br>Biological Evaluation of Benzo[c]heterocyclic Compounds against SHP2
%A 冯勃
%A 陈晓禹
%A RajendranSatheeshkumar
%A 王文龙
%J Hans Journal of Medicinal Chemistry
%P 79-83
%@ 2331-8295
%D 2020
%I Hans Publishing
%R 10.12677/HJMCe.2020.83009
%X 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 (IC<sub>50</sub> = 26.22 μM)对SHP2显示了中等强度的抑制活性。<br />
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 IC<sub>50</sub> of 26.22 μM against SHP2.
%K 苯并五元杂环化合物，SHP2<sup>PTP</sup>，抑制剂，构效关系<br>Benzo[c]heterocyclic Compounds
%K SHP2
%K Inhibitors
%K Structure-Activity Relationships (SARs)
%U http://www.hanspub.org/journal/PaperInformation.aspx?PaperID=37127