Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors

WL Wang, C Huang, LX Gao, CL Tang, JQ Wang…

Index: Wang, Wen-Long; Huang, Chao; Gao, Li-Xin; Tang, Chun-Lan; Wang, Jun-Qing; Wu, Min-Chen; Sheng, Li; Chen, Hai-Jun; Nan, Fa-Jun; Li, Jing-Ya; Li, Jia; Feng, Bainian Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 8 p. 1889 - 1894

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Citation Number: 6

Abstract

Abstract A series of bis-aromatic amides was designed, synthesized, and evaluated as a new class of inhibitors with IC 50 values in the micromolar range against protein tyrosine phosphatase 1B (PTP1B). Among them, compound 15 displayed an IC 50 value of 2.34±0.08 μM with 5-fold preference over TCPTP. More importantly, the treatment of CHO/HIR cells with compound 15 resulted in increased phosphorylation of insulin ...