Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors

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

Research output: Contribution to journalArticlepeer-review

64 Scopus citations


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 3 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma.

Original languageEnglish (US)
Pages (from-to)3706-3712
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Issue number14
StatePublished - Jul 15 2006

All Science Journal Classification (ASJC) codes

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


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