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RESEARCH PRODUCT

The development of benzimidazoles as selective rho kinase inhibitors

Yan YinE. Hampton SessionsBozena FrackowiakClaudia RuizBo WangPhilip LograssoThomas SchröterJennifer PocasLi LinSarwat ChowdhuryMichael D. CameronYen Ting ChenYangbo FengMichael P. SmolinskiThomas D. Bannister

subject

Serine/threonine-specific protein kinaserho-Associated KinasesMAP kinase kinase kinaseChemistryKinaseOrganic ChemistryClinical BiochemistryPharmaceutical ScienceGlaucomaChromanMitogen-activated protein kinase kinaseBiochemistryBenzimidazoleBiochemistryDrug DiscoveryROCKMolecular MedicineBenzimidazolesCyclin-dependent kinase 9Protein kinase ARho KinaseProtein Kinase InhibitorsMolecular BiologyRho-associated protein kinaseProtein kinase C

description

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)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).

yearjournalcountryeditionlanguage
2010-03-01Bioorganic & Medicinal Chemistry Letters : a tetrahedron publication for the rapid dissemination of preliminary communication and all aspects of bioorganic chemistry, medicinal chemistry and related disciplines
10.1016/j.bmcl.2010.01.124https://doi.org/10.1016/j.bmcl.2010.01.124