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