| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368973 | Bioorganic & Medicinal Chemistry Letters | 2015 | 4 Pages |
Abstract
The discovery, synthesis, and characterization of 9H-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.
Graphical abstractThe discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kurt Zimmermann, Xiaopeng Sang, Harold A. Mastalerz, Walter L. Johnson, Guifen Zhang, Qingjie Liu, Douglas Batt, Louis J. Lombardo, Dinesh Vyas, George L. Trainor, John S. Tokarski, Matthew V. Lorenzi, Dan You, Marco M. Gottardis, Jonathan Lippy,