| Literature DB >> 14592481 |
Zhili Xin1, Gang Liu, Cele Abad-Zapatero, Zhonghua Pei, Bruce G Szczepankiewicz, Xiaofeng Li, Tianyuan Zhang, Charles W Hutchins, Philip J Hajduk, Stephen J Ballaron, Michael A Stashko, Thomas H Lubben, James M Trevillyan, Michael R Jirousek.
Abstract
Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.Entities:
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Year: 2003 PMID： 14592481 DOI： 10.1016/j.bmcl.2003.08.064
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823