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

Jagabandhu Das, Chunjian Liu, Robert V. Moquin, James Lin, Joseph A. Furch, Steven H. Spergel, 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

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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.

Original languageEnglish (US)
Pages (from-to)2411-2415
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number9
DOIs
StatePublished - May 1 2006

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Das, J., Liu, C., Moquin, R. V., Lin, J., Furch, J. A., Spergel, S. H., McIntyre, K. W., Shuster, D. J., O'Day, K. D., Penhallow, B., Hung, C. Y., Kanner, S. B., Lin, T. A., Dodd, J. H., Barrish, J. C., & Wityak, J. (2006). Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(9), 2411-2415. https://doi.org/10.1016/j.bmcl.2006.01.115