794525-56-7Relevant academic research and scientific papers
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors
Zhao, Hongyu,Liu, Gang,Xin, Zhili,Serby, Michael D.,Pei, Zhonghua,Szczepankiewicz, Bruce G.,Hajduk, Philip J.,Abad-Zapatero, Cele,Hutchins, Charles W.,Lubben, Thomas H.,Ballaron, Stephen J.,Haasch, Deanna L.,Kaszubska, Wiweka,Rondinone, Cristina M.,Trevillyan, James M.,Jirousek, Michael R.
, p. 5543 - 5546 (2007/10/03)
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. 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.
