Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole

Tiansheng Wang,John P. Duffy,Jian Wang,Summer Halas,Francesco G. Salituro,Albert Pierce,Harmon Zuccola,James R. Black,James K. Hogan,Scott Jepson,Dina Shlyakter,Sudipta Mahajan,Yong Gu,Thomas Hoock,Mark Wood,Brinley Furey,J. Daniel Frantz,Lisa M. Dauffenbach,Ursula A. Germann,Bin Fan,Mark Namchuk,Youssef L. Bennani,Mark Ledeboer

Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole

2009

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.

Keywords:

Enzyme
Biochemistry
Signal transduction
Janus kinase 2
Organic chemistry
Enzyme inhibitor
Chemistry
Transferase
In vivo
Stereochemistry
Chemical synthesis
In vitro
Biological activity

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