氨基苯甲酸衍生物抑制SHP2活性研究
Biological Evaluation of Aminobenzoic Acid Derivatives against SHP2
DOI: 10.12677/HJMCe.2021.92011, PDF,    科研立项经费支持
作者: 孟祥东, Rajendran Satheeshkumar, 王文龙：江南大学药学院，江苏 无锡
关键词: SHP2；抑制剂；氨基苯甲酸；构效关系；SHP2； Inhibitors； Aminobenzoic Acid； Structure-Activity Relationships (SARs)
摘要: 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。
Abstract: 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.
文章引用：孟祥东, RajendranSatheeshkumar, 王文龙. 氨基苯甲酸衍生物抑制SHP2活性研究[J]. 药物化学, 2021, 9(2): 87-93. https://doi.org/10.12677/HJMCe.2021.92011

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