The development of benzimidazoles as selective rho kinase inhibitors

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 (IC 50

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1939-1943
Hauptverfasser: Sessions, E. Hampton, Smolinski, Michael, Wang, Bo, Frackowiak, Bozena, Chowdhury, Sarwat, Yin, Yan, Chen, Yen Ting, Ruiz, Claudia, Lin, Li, Pocas, Jennifer, Schröter, Thomas, Cameron, Michael D., LoGrasso, Philip, Feng, Yangbo, Bannister, Thomas D.
Format: Artikel
Sprache:eng
Schlagworte:
Benzimidazole
Benzimidazoles - pharmacology
Biological and medical sciences
Chroman
Eye
Glaucoma
Medical sciences
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Rho Kinase
rho-Associated Kinases - antagonists & inhibitors
ROCK
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Zusammenfassung: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 (IC 50
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.124