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