1346168-57-7Relevant articles and documents
An Improved Synthesis of the Free Base and Diglycolate Salt of CEP-33779; A Janus Kinase 2 Inhibitor
Levy, Daniel V.,Sclafani, Joseph A.,Bakale, Roger P.
, p. 2085 - 2091 (2016/12/24)
CEP-33779 is a triazole that has been reported to show highly selective inhibition of Janus kinase 2 (JAK2). An efficient process to form CEP-33779 will be presented that uses multiple palladium couplings to provide the drug substance in a convergent mann
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of janus kinase 2 for use in anticancer therapy: Discovery of CEP-33779
Dugan, Benjamin J.,Gingrich, Diane E.,Mesaros, Eugen F.,Milkiewicz, Karen L.,Curry, Matthew A.,Zulli, Allison L.,Dobrzanski, Pawel,Serdikoff, Cynthia,Jan, Mahfuza,Angeles, Thelma S.,Albom, Mark S.,Mason, Jennifer L.,Aimone, Lisa D.,Meyer, Sheryl L.,Huang, Zeqi,Wells-Knecht, Kevin J.,Ator, Mark A.,Ruggeri, Bruce A.,Dorsey, Bruce D.
, p. 5243 - 5254 (2012/09/21)
Members of the JAK family of nonreceptor tyrosine kinases play a critical role in the growth and progression of many cancers and in inflammatory diseases. JAK2 has emerged as a leading therapeutic target for oncology, providing a rationale for the development of a selective JAK2 inhibitor. A program to optimize selective JAK2 inhibitors to combat cancer while reducing the risk of immune suppression associated with JAK3 inhibition was undertaken. The structure-activity relationships and biological evaluation of a novel series of compounds based on a 1,2,4-triazolo[1,5-a]pyridine scaffold are reported. Para substitution on the aryl at the C8 position of the core was optimum for JAK2 potency (17). Substitution at the C2 nitrogen position was required for cell potency (21). Interestingly, meta substitution of C2-NH-aryl moiety provided exceptional selectivity for JAK2 over JAK3 (23). These efforts led to the discovery of CEP-33779 (29), a novel, selective, and orally bioavailable inhibitor of JAK2.
