Design and synthesis of tricyclic cores for kinase inhibition

…, B Fiamengo, J Edmunds, A Ericsson, K Frank…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 3 p. 693 - 698

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Citation Number: 7

Abstract

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 ...