The synthesis and evaluation of indolylureas as PKCα inhibitors

…, O Barker, KD Greis, S Zhou, E Dolan, GF Davis

文献索引：Djung, Jane F.; Mears, Richard. J.; Montalbetti, Christian A.G.N.; Coulter, Thomas S.; Golebiowski, Adam; Carr, Andrew N.; Barker, Oliver; Greis, Kenneth D.; Zhou, Songtao; Dolan, Elizabeth; Davis, Gregory F. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 8 p. 2742 - 2750

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被引用次数: 3

摘要

PKCα and PKA have crucial but opposing roles in the regulation of calcium handling within myocytes. Identification of compounds that inhibit PKCα, but not PKA, are potential therapeutic targets for the treatment of heart disease. The synthesis of indolylureas are described, and a compound displaying nanomolar inhibition towards PKCα with significant selectivity over PKA has been identified.