%0 Journal Article
%T 氨基苯甲酸衍生物抑制SHP2活性研究<br>Biological Evaluation of Aminobenzoic Acid Derivatives against SHP2
%A 孟祥东
%A RajendranSatheeshkumar
%A 王文龙
%J Hans Journal of Medicinal Chemistry
%P 87-93
%@ 2331-8295
%D 2021
%I Hans Publishing
%R 10.12677/HJMCe.2021.92011
%X 目前，SHP2抑制剂还存在着生物利用度低等问题，需要一些结构新颖的SHP2抑制剂。本文为拓展SHP2抑制剂的结构多样性，合成了18个氨基苯甲酸衍生物，其中3-(5-甲基呋喃-2-羧酰胺基)苯甲酸(化合物15)在50 mM浓度下表现了48.51%的抑制率，构效关系分析结果表明，羧基有利于抑制SHP2活性，为基于片段的SHP2抑制剂研究工作奠定了一定的基础。<br />
SHP2 inhibitors also have problems such as low bioavailability, and SHP2 inhibitors with novel structures are needed. In order to expand the structural diversity of SHP2 inhibitors, 18 amino-benzoic acid derivatives were synthesized. Among them, 3-(5-methylfuran-2-carboxamido)benzoic acid (Compound 15) showed 48.51% inhibitory rate at the concentration of 50 mM. The struc-ture-activity relationship analysis results show that the carboxyl group has positive influence on the activity against SHP2 and can be used as small fragments for subsequent development of SHP2 in-hibitors.
%K SHP2，抑制剂，氨基苯甲酸，构效关系<br>SHP2
%K Inhibitors
%K Aminobenzoic Acid
%K Structure-Activity Relationships (SARs)
%U http://www.hanspub.org/journal/PaperInformation.aspx?PaperID=42783