Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity

A series of phidianidine B derivatives were synthesized by introducing various heterocyclic rings. Their inhibitory effects on PTP1B and other PTPs (TCPTP, SHP1, SHP2 and LAR) were evaluated. A majority of them displayed significant inhibitory potency and specific selectivity over PTP1B. The SAR and molecular docking analysis were also described.

Graphical abstractFunction-oriented synthesis of phidianidine B derivatives was accomplished, their specific inhibitory effects on PTP1B, the SAR and molecular docking analysis were described.Figure optionsDownload full-size imageDownload as PowerPoint slide