The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors

J Tang, KE Lackey, SH Dickerson

Index: Tang, Jun; Lackey, Karen E.; Dickerson, Scott H. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 1 p. 66 - 70

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Citation Number: 5

Abstract

A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC50= 5.1, 16.6 nM) and cellular assay (IC50= 0.2, 0.2 μM), but also had an outstanding selectivity profile against other kinases.