Synthesis and Structure− Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D

K Bravo-Altamirano, KM George…

Index: Bravo-Altamirano, Karla; George, Kara M.; Frantz, Marie-Celine; Lavalle, Courtney R.; Tandon, Manuj; Leimgruber, Stephanie; Sharlow, Elizabeth R.; Lazo, John S.; Wang, Q. Jane; Wipf, Peter ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 2 p. 154 - 159

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Citation Number: 19

Abstract

Protein kinase D (PKD) is a member of a novel family of serine/threonine kinases that regulate fundamental cellular processes. PKD is implicated in the pathogenesis of several diseases, including cancer. Progress in understanding the biological functions and therapeutic potential of PKD has been hampered by the lack of specific inhibitors. The benzoxoloazepinolone CID755673 was recently identified as the first potent and selective ...