Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
作者信息
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
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jul 15;16(14):3706-12. doi: 10.1016/j.bmcl.2006.04.060. Epub 2006 May 6.
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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