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

…, DE Gingrich, EF Mesaros, KL Milkiewicz…

Index: 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. Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5243 - 5254

Full Text: HTML

Citation Number: 23

Abstract

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 ...