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Design, Synthesis, and Biological Evaluation of PKD Inhibitors
Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA
Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA
Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA
* Author to whom correspondence should be addressed.
Received: 17 February 2011; in revised form: 1 April 2011 / Accepted: 19 April 2011 / Published: 21 April 2011
Abstract: Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated.
Keywords: protein kinase D; small molecule inhibitor; benzothienothiazepinone; pyrimidines; CID755673; thiazepinothiophenopyrimidinone
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George, K.M.; Frantz, M.-C.; Bravo-Altamirano, K.; LaValle, C.R.; Tandon, M.; Leimgruber, S.; Sharlow, E.R.; Lazo, J.S.; Wang, Q.J.; Wipf, P. Design, Synthesis, and Biological Evaluation of PKD Inhibitors. Pharmaceutics 2011, 3, 186-228.
George KM, Frantz M-C, Bravo-Altamirano K, LaValle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P. Design, Synthesis, and Biological Evaluation of PKD Inhibitors. Pharmaceutics. 2011; 3(2):186-228.
George, Kara M.; Frantz, Marie-Céline; Bravo-Altamirano, Karla; LaValle, Courtney R.; Tandon, Manuj; Leimgruber, Stephanie; Sharlow, Elizabeth R.; Lazo, John S.; Wang, Q. Jane; Wipf, Peter. 2011. "Design, Synthesis, and Biological Evaluation of PKD Inhibitors." Pharmaceutics 3, no. 2: 186-228.