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  • Title: Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.
    Author: Friedman M, Frank KE, Aguirre A, Argiriadi MA, Davis H, Edmunds JJ, George DM, George JS, Goedken E, Fiamengo B, Hyland D, Li B, Murtaza A, Morytko M, Somal G, Stewart K, Tarcsa E, Van Epps S, Voss J, Wang L, Woller K, Wishart N.
    Journal: Bioorg Med Chem Lett; 2015 Oct 15; 25(20):4399-404. PubMed ID: 26372653.
    Abstract:
    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.
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