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Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors

2004; Elsevier BV; Volume: 14; Issue: 22 Linguagem: Inglês

10.1016/j.bmcl.2004.08.063

1464-3405

Hongyu Zhao, Gang Liu, Zhili Xin, Michael D. Serby, Zhonghua Pei, Bruce G. Szczepankiewicz, Philip J. Hajduk, Cele Abad‐Zapatero, Charles W. Hutchins, Thomas Lübben, Stephen J. Ballaron, Deanna L. Haasch, Wiweka Kaszubska, Cristina M. Rondinone, James M. Trevillyan, Michael R. Jirousek,

Cytokine Signaling Pathways and Interactions

Guided by X-ray crystallography, we have extended the structure–activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.