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Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck

2003; Elsevier BV; Volume: 13; Issue: 22 Linguagem: Inglês

10.1016/j.bmcl.2003.08.054

1464-3405

John Wityak, Jagabandhu Das, Robert V. Moquin, Zhongqi Shen, James C. Lin, Ping Chen, Arthur M. Doweyko, Sidney Pitt, Suhong Pang, Ding Ren Shen, Qiong Fang, H. Fex, Gary L. Schieven, Steven B. Kanner, Joel C. Barrish,

14-3-3 protein interactions

A novel series of 2-amino-5-carboxamidothiazoles were identified as inhibitors of Lck. Structure-activity studies demonstrate the structural requirements for potent Lck activity. Cyclopropylamide 11d is a potent Lck inhibitor having sub-micromolar activity in a PBL proliferation assay.