The development of benzimidazoles as selective rho kinase inhibitors
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 10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
Sessions, E. Hampton,Smolinski, Michael,Wang, Bo,Frackowiak, Bozena,Chowdhury, Sarwat,Yin, Yan,Chen, Yen Ting,Ruiz, Claudia,Lin, Li,Pocas, Jennifer,Schr?ter, Thomas,Cameron, Michael D.,LoGrasso, Philip,Feng, Yangbo,Bannister, Thomas D.
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p. 1939 - 1943
(2010/09/03)
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.