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ID: ALA1764955

Journal: Bioorg Med Chem

Title: The synthesis and evaluation of indolylureas as PKCα inhibitors.

Authors: Djung JF, Mears RJ, Montalbetti CA, Coulter TS, Golebiowski A, Carr AN, Barker O, Greis KD, Zhou S, Dolan E, Davis GF.

Abstract: 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.

CiteXplore: 21435888

DOI: 10.1016/j.bmc.2011.02.036