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 ,
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.
