Download Mendeley2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Ledeboer, M.W., Pierce, A.C., Duffy, J.P., Gao, H., Messersmith, D., Salituro, F.G., Nanthakumar, S., Come, J., Zuccola, H.J., Swenson, L., Shlyakter, D., Mahajan, S., Hoock, T., Fan, B., Tsai, W.J., Kolaczkowski, E., Carrier, S., Hogan, J.K., Zessis, R., Pazhanisamy, S., Bennani, Y.L.(2009) Bioorg Med Chem Lett 19: 6529-6533
- PubMed: 19857967
- DOI: https://doi.org/10.1016/j.bmcl.2009.10.053
- Primary Citation of Related Structures:
3IO7, 3IOK - PubMed Abstract:
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.
Organizational Affiliation:
Vertex Pharmaceuticals Inc, Cambridge, MA 02139-4242, United States. mark_ledeboer@vrtx.com
