Literature DB >> 16481166

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

Jagabandhu Das1, Chunjian Liu, Robert V Moquin, James Lin, Joseph A Furch, Steven H Spergel, Arthur M Doweyko, Kim W McIntyre, David J Shuster, Kathleen D O'Day, Becky Penhallow, Chen-Yi Hung, Steven B Kanner, Tai-An Lin, John H Dodd, Joel C Barrish, John Wityak.   

Abstract

A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 2 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo.

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Year:  2006        PMID: 16481166     DOI: 10.1016/j.bmcl.2006.01.115

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


  5 in total

1.  Discovery of potent inhibitors for interleukin-2-inducible T-cell kinase: structure-based virtual screening and molecular dynamics simulation approaches.

Authors:  Chandrasekaran Meganathan; Sugunadevi Sakkiah; Yuno Lee; Jayavelu Venkat Narayanan; Keun Woo Lee
Journal:  J Mol Model       Date:  2012-09-27       Impact factor: 1.810

2.  Targeting Interleukin-2-Inducible T-cell Kinase (ITK) in T-Cell Related Diseases.

Authors:  Yiming Zhong; Amy J Johnson; John C Byrd; Jason A Dubovsky
Journal:  Postdoc J       Date:  2014-06

3.  A practically simple, catalyst free and scalable synthesis of N-substituted ureas in water.

Authors:  Lata Tiwari; Varun Kumar; Bhuvesh Kumar; Dinesh Mahajan
Journal:  RSC Adv       Date:  2018-06-13       Impact factor: 4.036

Review 4.  ITK inhibitors in inflammation and immune-mediated disorders.

Authors:  Nisebita Sahu; Avery August
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

5.  Differential sensitivity to Itk kinase signals for T helper 2 cytokine production and chemokine-mediated migration.

Authors:  Nisebita Sahu; Cynthia Mueller; Angela Fischer; Avery August
Journal:  J Immunol       Date:  2008-03-15       Impact factor: 5.422

  5 in total

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