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Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors |
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| Authors: | Das Jagabandhu Furch Joseph A Liu Chunjian Moquin Robert V Lin James Spergel Steven H McIntyre Kim W Shuster David J O'Day Kathleen D Penhallow Becky Hung Chen-Yi Doweyko Arthur M Kamath Amrita Zhang Hongjian Marathe Punit Kanner Steven B Lin Tai-An Dodd John H Barrish Joel C Wityak John |
| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. jagabandhu.das@bms.com |
| 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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