Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors |
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| Affiliation: | 1. Laboratory of Physiology, School of Life Science, East China Normal University, Shanghai 200062, China;2. National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China |
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| Abstract: | A series of bis-aromatic amides was designed, synthesized, and evaluated as a new class of inhibitors with IC50 values in the micromolar range against protein tyrosine phosphatase 1B (PTP1B). Among them, compound 15 displayed an IC50 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 receptor (IR), which suggested extensive cellular activity of compound 15. These results provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
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| Keywords: | Bis-aromatic amides PTP1B inhibitors Selectivity Cellular activity Structure–activity relationships (SARs) |
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