2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo [d] imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor

…, W Huang, A Thorarensen, L Xing, NL Caspers…

Index: Trujillo, John I.; Kiefer, James R.; Huang, Wei; Thorarensen, Atli; Xing, Li; Caspers, Nicole L.; Day, Jacqueline E.; Mathis, Karl J.; Kretzmer, Kuniko K.; Reitz, Beverley A.; Weinberg, Robin A.; Stegeman, Roderick A.; Wrightstone, Ann; Christine, Lori; Compton, Robert; Li, Xiong Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 908 - 911

Full Text: HTML

Citation Number: 37

Abstract

The inhibition of PKC-ζ has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H indazol-3-yl)-1H-benzo [d] imidazoles with initial high crossover to CDK-2 has been optimized to afford potent and selective inhibitors of protein kinase c-zeta (PKC-ζ). The determination of the crystal structures of key inhibitor: CDK-2 complexes informed the design and analysis of the series. The most ...