Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56lck inhibitors

A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) 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. (C) 2003 Elsevier Ltd. All rights reserved.