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氨基苯甲酸衍生物抑制SHP2活性研究
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Abstract:
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。
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.
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