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2 results on '"Johnson, Walter L."'

1. 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Author

Zimmermann, Kurt, Sang, Xiaopeng, Mastalerz, Harold A., Johnson, Walter L., Zhang, Guifen, Liu, Qingjie, Batt, Douglas, Lombardo, Louis J., Vyas, Dinesh, Trainor, George L., Tokarski, John S., Lorenzi, Matthew V., You, Dan, Gottardis, Marco M., Lippy, Jonathan, Khan, Javed, Sack, John S., and Purandare, Ashok V.

Subjects
*ENZYME inhibitors, *CARBOXAMIDES, *CARBAZOLE, *JANUS kinases, *CHEMICAL synthesis, *DRUG development
Abstract

The discovery, synthesis, and characterization of 9 H -carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed. Optimization for JAK family selectivity led to compounds 14 and 21 , with greater than 45-fold selectivity for JAK2 over all other members of the JAK kinase family. [ABSTRACT FROM AUTHOR]

Published
2015
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2. Pyrrolo[1,2-f]triazines as JAK2 inhibitors: Achieving potency and selectivity for JAK2 over JAK3

Author

Harikrishnan, Lalgudi S., Kamau, Muthoni G., Wan, Honghe, Inghrim, Jennifer A., Zimmermann, Kurt, Sang, Xiaopeng, Mastalerz, Harold A., Johnson, Walter L., Zhang, Guifen, Lombardo, Louis J., Poss, Michael A., Trainor, George L., Tokarski, John S., Lorenzi, Matthew V., You, Dan, Gottardis, Marco M., Baldwin, Kathy F., Lippy, Jonathan, Nirschl, David S., and Qiu, Ruhui

Subjects
*TRIAZINES, *ENZYME inhibitors, *MYELOPROLIFERATIVE neoplasms, *PROTEIN kinases, *MOLECULAR biology, *GENETIC transcription, *ENZYME activation
Abstract

Abstract: SAR studies of pyrrolo[1,2-f]triazines as JAK2 inhibitors is presented. Achieving JAK2 inhibition selectively over JAK3 is discussed. [Copyright &y& Elsevier]

Published
2011
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