1169687-29-9Relevant articles and documents
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
Ledeboer, Mark W.,Pierce, Albert C.,Duffy, John P.,Gao, Huai,Messersmith, David,Salituro, Francesco G.,Nanthakumar, Suganthini,Come, Jon,Zuccola, Harmon J.,Swenson, Lora,Shlyakter, Dina,Mahajan, Sudipta,Hoock, Thomas,Fan, Bin,Tsai, Wan-Jung,Kolaczkowski, Elaine,Carrier, Scott,Hogan, James K.,Zessis, Richard,Pazhanisamy,Bennani, Youssef L.
scheme or table, p. 6529 - 6533 (2010/05/18)
Constitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.
