Literature DB >> 20138510

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Marc Gerspacher1, Pascal Furet, Carole Pissot-Soldermann, Christoph Gaul, Philipp Holzer, Eric Vangrevelinghe, Marc Lang, Dirk Erdmann, Thomas Radimerski, Catherine H Regnier, Patrick Chene, Alain De Pover, Francesco Hofmann, Fabienne Baffert, Thomas Buhl, Reiner Aichholz, Francesca Blasco, Ralf Endres, Jörg Trappe, Peter Drueckes.   

Abstract

A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure-activity relationship data are also provided. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20138510     DOI: 10.1016/j.bmcl.2010.01.069

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.

Authors:  Maninder Kaur; Pankaj Kumar Singh; Manjinder Singh; Renu Bahadur; Om Silakari
Journal:  Mol Divers       Date:  2017-11-14       Impact factor: 2.943

2.  Dual inhibitors of Janus kinase 2 and 3 (JAK2/3): designing by pharmacophore- and docking-based virtual screening approach.

Authors:  Haneesh Jasuja; Navriti Chadha; Maninder Kaur; Om Silakari
Journal:  Mol Divers       Date:  2014-01-11       Impact factor: 2.943

Review 3.  The recent medicinal chemistry development of Jak2 tyrosine kinase small molecule inhibitors.

Authors:  R Baskin; A Majumder; P P Sayeski
Journal:  Curr Med Chem       Date:  2010       Impact factor: 4.530

  3 in total

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