1201186-94-8Relevant articles and documents
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors
Friedman, Michael,Frank, Kristine E.,Aguirre, Ana,Argiriadi, Maria A.,Davis, Heather,Edmunds, Jeremy J.,George, Dawn M.,George, Jonathan S.,Goedken, Eric,Fiamengo, Bryan,Hyland, Deborah,Li, Bin,Murtaza, Anwar,Morytko, Michael,Somal, Gagandeep,Stewart, Kent,Tarcsa, Edit,Van Epps, Stacy,Voss, Jeffrey,Wang, Lu,Woller, Kevin,Wishart, Neil
, p. 4399 - 4404 (2015/10/12)
Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that 1-cyclohexyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (12) had Jak inhibitory activity. Herein we describe our initial efforts to develop orally bioavailable analogs of 12 with improved selectivity of Jak1 over Jak2.