| Literature DB >> 24684845 |
Wen-Long Wang1, Chao Huang2, Li-Xin Gao3, Chun-Lan Tang3, Jun-Qing Wang2, Min-Chen Wu2, Li Sheng3, Hai-Jun Chen3, Fa-Jun Nan3, Jing-Ya Li3, Jia Li4, Bainian Feng5.
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.Entities:
Keywords: Bis-aromatic amides; Cellular activity; PTP1B inhibitors; Selectivity; Structure–activity relationships (SARs)
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Year: 2014 PMID： 24684845 DOI： 10.1016/j.bmcl.2014.03.015
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823