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

Bioorg Med Chem Lett

Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA.

Published: July 2006

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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http://dx.doi.org/10.1016/j.bmcl.2006.04.060DOI Listing

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