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

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

  • Bioorg Med Chem Lett. 2006 Jul 15;16(14):3706-12. doi: 10.1016/j.bmcl.2006.04.060.
Jagabandhu Das 1,  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
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. jagabandhu.das@bms.com
PMID: 16682193 DOI: 10.1016/j.bmcl.2006.04.060
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 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.

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