Title of article
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
Author/Authors
Jagabandhu Das، نويسنده , , Joseph A. Furch، نويسنده , , Chunjian Liu، نويسنده , , Robert V. Moquin، نويسنده , , Ming-Ji James Lin، نويسنده , , Steven H. Spergel، نويسنده , , Kim W. McIntyre، نويسنده , , David J. Shuster، نويسنده , , Kathleen D. O’Day، نويسنده , , Becky Penhallow، نويسنده , , Chen-Yi Hung، نويسنده , , Arthur M. Doweyko، نويسنده , , Amrita Kamath، نويسنده , , Hongjian Zhang، نويسنده , , Punit Marathe، نويسنده , , Steven B. Kanner، نويسنده , , Tai-An Lin، نويسنده , , John H. Dodd، نويسنده , , Joel C. Barrish، نويسنده , , John Wityak، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
7
From page
3706
To page
3712
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.
Keywords
Amino-(thioaryl)thiazoles , Selective Itk inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797061
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