| Literature DB >> 25987372 |
Kurt Zimmermann1, Xiaopeng Sang2, Harold A Mastalerz2, Walter L Johnson2, Guifen Zhang2, Qingjie Liu3, Douglas Batt3, Louis J Lombardo3, Dinesh Vyas2, George L Trainor3, John S Tokarski3, Matthew V Lorenzi3, Dan You3, Marco M Gottardis3, Jonathan Lippy3, Javed Khan3, John S Sack3, Ashok V Purandare3.
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.Entities:
Keywords: JAK; JAK family selectivity; JAK1; JAK2; JAK3; Myeloproliferative disorders; Myeloproliferative neoplasms; TYK2
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Year: 2015 PMID： 25987372 DOI： 10.1016/j.bmcl.2015.04.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823