title: The synthesis and evaluation of indolylureas as PKCα inhibitors.
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.
authors: Procter & Gamble Pharmaceuticals Inc., Health Care Research Center, Mason, OH 45040-9462, USA.
authors: Jane F
authors: JF
authors: Djung
authors: Richard J
authors: RJ
authors: Mears
authors: Christian A G N
authors: CA
authors: Montalbetti
authors: Thomas S
authors: TS
authors: Coulter
authors: Adam
authors: A
authors: Golebiowski
authors: Andrew N
authors: AN
authors: Carr
authors: Oliver
authors: O
authors: Barker
authors: Kenneth D
authors: KD
authors: Greis
authors: Songtao
authors: S
authors: Zhou
authors: Elizabeth
authors: E
authors: Dolan
authors: Gregory F
authors: GF
authors: Davis
mesh_terms: D017868:Cyclic AMP-Dependent Protein Kinases; D006331:Heart Diseases / Q000188:drug therapy; D006801:Humans; D051571:Protein Kinase C-alpha / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis*; D014508:Urea / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D014508:Urea; D017868:Cyclic AMP-Dependent Protein Kinases; D051571:Protein Kinase C-alpha