Title of article :
Molecular design, synthesis, and structure–Activity relationships leading to the potent and selective p56lck inhibitor BMS-243117
Author/Authors :
Jagabandhu Das، نويسنده , , Ming-Ji James Lin، نويسنده , , Robert V. Moquin، نويسنده , , Zhongqi Shen، نويسنده , , Steven H. Spergel، نويسنده , , John Wityak، نويسنده , , Arthur M. Doweyko، نويسنده , , Henry F. DeFex، نويسنده , , Qiong Fang، نويسنده , , Suhong Pang، نويسنده , , Sidney Pitt، نويسنده , , Ding Ren Shen، نويسنده , , Gary L. Schieven، نويسنده , , Joel C. Barrish، نويسنده ,
Abstract :
A series of structurally novel benzothiazole based small molecule inhibitors of p56lck were prepared to elucidate their structure–activity relationships (SARs), selectivity and cell activity in the T-cell proliferation assay. BMS-243117 (compound 2) is identified as a potent, and selective Lck inhibitor with good cellular activity (IC50=1.1 μM) against T-cell proliferation.
