436864-41-4Relevant academic research and scientific papers
Selective protein tyrosine phosphatatase inhibitors
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, (2008/06/13)
Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.
Selective protein tyrosine phosphatase 1B inhibitors: Targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands
Liu, Gang,Xin, Zhili,Liang, Heng,Abad-Zapatero, Cele,Hajduk, Philip J.,Janowick, David A.,Szczepankiewicz, Bruce G.,Pei, Zhonghua,Hutchins, Charles W.,Ballaron, Stephen J.,Stashko, Michael A.,Lubben, Thomas H.,Berg, Cathy E.,Rondinone, Cristina M.,Trevillyan, James M.,Jirousek, Michael R.
, p. 3437 - 3440 (2007/10/03)
Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling cascades. We identified several salicylic acid-based ligands for the second phosphotyrosine binding site of PTP1B using a NMR-based screening. Structure-based linking with a catalytic site-directed oxalylarylaminobenzoic acid-based pharmacophore led to the identification of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity over the highly homologous T-cell PTPase (TCPTP) and high selectivity over other phosphatases.
Potent, selective inhibitors of protein tyrosine phosphatase 1B
Xin, Zhili,Oost, Thorsten K.,Abad-Zapatero, Cele,Hajduk, Philip J.,Pei, Zhonghua,Szczepankiewicz, Bruce G.,Hutchins, Charles W.,Ballaron, Steve J.,Stashko, Mike A.,Lubben, Tom,Trevillyan, James M.,Jirousek, Mike R.,Liu, Gang
, p. 1887 - 1890 (2007/10/03)
We have previously reported a novel series of oxalyl-aryl-amino benzoic acid-based, catalytic site-directed, competitive, reversible protein tyrosine phosphatase 1B (PTP1B) inhibitors. With readily access to key intermediates, we utilized a solution phase
Selective protein tyrosine phosphatatase inhibitors
-
, (2008/06/13)
Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.
Amino (oxo) acetic acid protein tyrosine phosphatase inhibitors
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, (2008/06/13)
Compounds of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
