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Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Bioorganic & medicinal chemistry letters 2004 Dec 20; 14(24):6061-6

Link to PubMed abstract

Chen P P, Norris D D, Das J J, Spergel S SH, Wityak J J, Leith L L, Zhao R R, Chen B BC, Pitt S S, Pang S S, Shen D DR, Zhang R R, De Fex H HF, Doweyko A AM, McIntyre K KW, Shuster D DJ, Behnia K K, Schieven G GL, Barrish J JC

Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ping.chen@bms.com

A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy.