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Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors |
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| Authors: | Chen Ping Norris Derek Das Jagabandhu Spergel Steven H Wityak John Leith Leslie Zhao Rulin Chen Bang-Chi Pitt Sidney Pang Suhong Shen Ding Ren Zhang Rosemary De Fex Henry F Doweyko Arthur M McIntyre Kim W Shuster David J Behnia Kamelia Schieven Gary L Barrish Joel C |
| Institution: | aDepartment of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA bDepartment of Immunology, Inflammation and Pulmonary Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA cDepartment of Macromolecular Structure, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA dDepartment of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA |
| Abstract: | 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. |
| Keywords: | Lck inhibitor pan-Src-family inhibitor |
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