Author/Authors :
Jagabandhu Das، نويسنده , , Robert V. Moquin، نويسنده , , Ming-Ji James Lin، نويسنده , , Chunjian Liu، 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 , , John Wityak، نويسنده ,
Abstract :
A series of structurally novel benzothiazole based small molecule inhibitors of p56lck was prepared to elucidate their structure–activity relationships (SAR), selectivity and cell activity in the T-cell proliferation assay. BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation.