131885-95-5Relevant articles and documents
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase
Wittman, Mark D.,Balasubramanian, Balu,Stoffan, Karen,Velaparthi, Upender,Liu, Pieying,Krishnanathan, Subramaniam,Carboni, Joan,Li, Aixin,Greer, Ann,Attar, Ricardo,Gottardis, Marco,Chang, Chiehying,Jacobson, Bruce,Sun, Yax,Hansel, Steven,Zoeckler, Mary,Vyas, Dolatrai M.
, p. 974 - 977 (2007/10/03)
A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency.
Benzimidazole C-2 heterocycles as kinase inhibitors
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Page/Page column 14-15, (2010/02/11)
Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer.
Cardiotonic Agents. Synthesis and Cardiovascular Properties of Novel 2-Arylbenzimidazoles and Azabenzimidazoles
Guengoer, Timur,Fouquet, Andre,Teulon, Jean-Marie,Provost, Daniel,Cazes, Michele,et al.
, p. 4455 - 4463 (2007/10/02)
Novel 2-arylbenzimidazoles and azabenzimidazoles were synthesized, and their inotropic action was evaluated.Changes in left ventricular pressure, dP/dt max, were measured as an index of cardiac contractility.The structural features that impart optimal inotropic activity are presented.The most potent compounds were evaluated orally in conscious dogs with implanted Konigsberg pressure transducers.To investigate the mechanism of action, the most potent compounds were tested for their calcium-sensitizing properties and their potential for the inhibition of phosphodiesterase.Two compounds, 1 and 41, showed interesting in vitro and oral activity without side effects.They have a more potent calcium-sensitizing effect than MCI-154 and are under further investigation.