1421338-19-3Relevant academic research and scientific papers
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.
Design and synthesis of tricyclic cores for kinase inhibition
Van Epps, Stacy,Fiamengo, Bryan,Edmunds, Jeremy,Ericsson, Anna,Frank, Kristine,Friedman, Michael,George, Dawn,George, Jonathan,Goedken, Eric,Kotecki, Brian,Martinez, Gloria,Merta, Philip,Morytko, Michael,Shekhar, Shashank,Skinner, Barbara,Stewart, Kent,Voss, Jeffrey,Wallace, Grier,Wang, Lu,Wishart, Neil
, p. 693 - 698 (2013/03/13)
Interest in therapeutic kinase inhibitors continues to grow beyond success in oncology. To date, ATP-mimetic kinase inhibitors have focused primarily on monocyclic and bicyclic heterocyclic cores. We sought to expand on the repertoire of potential cores for kinase inhibition by exploring tricyclic variants of classical bicyclic hinge binding motifs such as pyrrolopyridine and pyrrolopyrazine. Herein we describe the syntheses of eight alternative tricyclic cores as well as in vitro screening results for representative kinases of potential therapeutic interest.
