Search Results - "Prokopowicz, Anthony S."

Three mechanistically distinct kinase assays compared: Measurement of intrinsic ATPase activity identified the most comprehensive set of ITK inhibitors by Kashem, Mohammed A, Nelson, Richard M, Yingling, Jeffrey D, Pullen, Steven S, Prokopowicz, 3rd, Anthony S, Jones, Jessi Wildeson, Wolak, John P, Rogers, George R, Morelock, Maurice M, Snow, Roger J, Homon, Carol Ann, Jakes, Scott

“…Numerous assay methods have been developed to identify small-molecule effectors of protein kinases, but no single method can be applied to all isolated…”
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Discovery of potent and selective PKC-θ inhibitors by Cywin, Charles L., Dahmann, Georg, Prokopowicz, Anthony S., Young, Erick R.R., Magolda, Ronald L., Cardozo, Mario G., Cogan, Derek A., DiSalvo, Darren, Ginn, John D., Kashem, Mohammed A., Wolak, John P., Homon, Carol A., Farrell, Thomas M., Grbic, Heather, Hu, Hanbo, Kaplita, Paul V., Liu, Lisa H., Spero, Denice M., Jeanfavre, Deborah D., O’Shea, Kathy M., White, Della M., Woska, Joseph R., Brown, Maryanne L.

“…An uHTS campaign was performed to identify selective inhibitors of PKC-θ. Initial triaging of the hit set based on selectivity and historical analysis led to…”
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Discovery of 2-Phenylamino-imidazo[4,5-h]isoquinolin-9-ones:  A New Class of Inhibitors of Lck Kinase by Snow, Roger J, Cardozo, Mario G, Morwick, Tina M, Busacca, Carl A, Dong, Yong, Eckner, Robert J, Jacober, Stephen, Jakes, Scott, Kapadia, Suresh, Lukas, Susan, Panzenbeck, Maret, Peet, Gregory W, Peterson, Jeffrey D, Prokopowicz, Anthony S, Sellati, Rosemarie, Tolbert, Robert M, Tschantz, Matt A, Moss, Neil

“…An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5‘-triphosphate competitive inhibitor of lck by high throughput screening. Initial…”
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Optimization of 2-Phenylaminoimidazo[4,5-h]isoquinolin-9-ones:  Orally Active Inhibitors of lck Kinase by Goldberg, Daniel R, Butz, Tanja, Cardozo, Mario G, Eckner, Robert J, Hammach, Abdelhakim, Huang, Jessica, Jakes, Scott, Kapadia, Suresh, Kashem, Mohammed, Lukas, Susan, Morwick, Tina M, Panzenbeck, Maret, Patel, Usha, Pav, Susan, Peet, Gregory W, Peterson, Jeffrey D, Prokopowicz, Anthony S, Snow, Roger J, Sellati, Rosemarie, Takahashi, Hidenori, Tan, Jonathan, Tschantz, Matt A, Wang, Xiao-Jun, Wang, Yong, Wolak, John, Xiong, Pla, Moss, Neil

“…The tyrosine kinase p56lck (lck) is essential for T cell activation; thus, inhibitors of lck have potential utility as autoimmune agents. Our initial…”
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Discovery and SAR of novel [1,6]Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK) by Cywin, Charles L, Zhao, Bao-Ping, McNeil, Daniel W, Hrapchak, Matt, Prokopowicz, Anthony S, Goldberg, Daniel R, Morwick, Tina M, Gao, Amy, Jakes, Scott, Kashem, Mohammed, Magolda, Ronald L, Soll, Richard M, Player, Mark R, Bobko, Mark A, Rinker, James, DesJarlais, Renee L, Winters, Michael P

“…The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity…”
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4-Trifloxy-9-SEM-β-Carboline:  Preparation and Synthetic Utility by Busacca, Carl A, Eriksson, Magnus C, Dong, Yong, Prokopowicz, Anthony S, Salvagno, Annette M, Tschantz, Matt A

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Isoquinolinone synthesis by SNAr reaction: a versatile route to imidazo[4,5-h]isoquinolin-9-ones by Snow, Roger J., Butz, Tanja, Hammach, Abdelhakim, Kapadia, Suresh, Morwick, Tina M., Prokopowicz, Anthony S., Takahashi, Hidenori, Tan, Jonathan D., Tschantz, Matt A., Wang, Xiao-Jun

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Isoquinolinone synthesis by S NAr reaction: a versatile route to imidazo[4,5- h]isoquinolin-9-ones by Snow, Roger J., Butz, Tanja, Hammach, Abdelhakim, Kapadia, Suresh, Morwick, Tina M., Prokopowicz, Anthony S., Takahashi, Hidenori, Tan, Jonathan D., Tschantz, Matt A., Wang, Xiao-Jun

“…Reaction of 2-chlorobenzonitriles with β-ketoesters in an S NAr reaction, followed by cyclization in acid provides a versatile route to isoquinolones. Starting…”
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Addition reactions of cyclic s-trans-enaminones with Grignard reagents by Shawe, Thomas T., Hansen, Darren B., Peet, Kelly Ann, Prokopowicz, Anthony S., Robinson, Patrice M., Cannon, Annatina, Dougherty, Kathleen E., Ross, Andrew A., Landino, Linda M.

“…Addition of Grignard reagents to s-trans-enaminones derived from 1,3-cycloalkanediones are described. In dichloromethane, addition of phenylmagnesium bromide…”
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New chemistry of cyclic, s- trans-enaminones: Addition of grignard reagents to enaminones derived from 2-methylcyclohexane-1,3-dione by Shawe, Thomas T., Landino, Linda M., Ross, Andrew A., Prokopowicz, Anthony S., Robinson, Patrice M., Cannon, Annatina

“…Grignard reagents add to cyclic s-trans enaminones to give the cycloalkenone after aqueous hydrolysis. In some cases a competitive double addition takes place…”
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