1. Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole
- Author
-
Scott Jepson, Youssef L. Bennani, Lisa M Dauffenbach, James K. Hogan, J. Daniel Frantz, Albert C. Pierce, Francesco G. Salituro, Bin Fan, Tiansheng Wang, Jian Wang, James Black, Mark Wood, Yong Gu, Brinley Furey, Harmon J. Zuccola, Dina Shlyakter, Thomas Hoock, Ursula A. Germann, Summer Halas, Sudipta Mahajan, Mark W. Ledeboer, Mark N. Namchuk, and John P. Duffy
- Subjects
Male ,Models, Molecular ,Indoles ,Protein Conformation ,Stereochemistry ,Lactams, Macrocyclic ,Molecular Conformation ,Mice, SCID ,Crystallography, X-Ray ,Chemical synthesis ,Rats, Sprague-Dawley ,Mice ,chemistry.chemical_compound ,In vivo ,Cell Line, Tumor ,hemic and lymphatic diseases ,Drug Discovery ,Animals ,Transferase ,Erythropoietin ,Protein Kinase Inhibitors ,Aza Compounds ,Mice, Inbred BALB C ,Janus kinase 2 ,biology ,Chemistry ,food and beverages ,Biological activity ,Janus Kinase 2 ,In vitro ,Rats ,biology.protein ,Molecular Medicine ,Signal transduction ,hormones, hormone substitutes, and hormone antagonists ,Derivative (chemistry) ,Signal Transduction - Abstract
The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further evaluated for its ability to block the EPO/JAK2 signaling cascade in vitro and in vivo.
- Published
- 2009