The development of benzimidazoles as selective rho kinase inhibitors

…, J Pocas, T Schröter, MD Cameron, P LoGrasso…

文献索引：Sessions, E. Hampton; Smolinski, Michael; Wang, Bo; Frackowiak, Bozena; Chowdhury, Sarwat; Yin, Yan; Chen, Yen Ting; Ruiz, Claudia; Lin, Li; Pocas, Jennifer; Schroeter, Thomas; Cameron, Michael D.; LoGrasso, Philip; Feng, Yangbo; Bannister, Thomas D. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 6 p. 1939 - 1943

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被引用次数: 16

摘要

Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC50< 10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).