Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole
journal contributionposted on 24.12.2009, 00:00 by Tiansheng Wang, John P. Duffy, Jian Wang, Summer Halas, Francesco G. Salituro, Albert C. Pierce, Harmon J. Zuccola, James R. Black, James K. Hogan, Scott Jepson, Dina Shlyakter, Sudipta Mahajan, Yong Gu, Thomas Hoock, Mark Wood, Brinley F. Furey, J. Daniel Frantz, Lisa M. Dauffenbach, Ursula A. Germann, Bin Fan, Mark Namchuk, Youssef L. Bennani, Mark W. Ledeboer
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.