1056877-62-3Relevant articles and documents
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors
Zimmermann, Kurt,Wittman, Mark D.,Saulnier, Mark G.,Velaparthi, Upender,Langley, David R.,Sang, Xiaopeng,Frennesson, David,Carboni, Joan,Li, Aixin,Greer, Ann,Gottardis, Marco,Attar, Ricardo M.,Yang, Zheng,Balimane, Praveen,Discenza, Lorell N.,Vyas, Dolatrai
scheme or table, p. 4075 - 4080 (2009/04/07)
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.
