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Velaparthi, Upender; Wittman, Mark; Liu, Peiying; Stoffan, Karen; Zimmermann, Kurt; Sang, Xiaopeng; Carboni, Joan; Li, Aixin; Attar, Ricardo; Gottardis, Marco; Greer, Ann; Chang, ChiehYing Y.; Jacobsen, Bruce L.; Sack, John S.; Sun, Yax; Langley, David R.; Balasubramanian, Balu; Vyas, Dolatrai
Bioorganic & medicinal chemistry letters, 04/2007, Letnik: 17, Številka: 8Journal Article
The discovery and synthesis of 3-(1 H-benzo dimidazol-2-yl)pyridin-2(1 H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) are presented. Installing amine containing side chains at the 4-position of pyridone ring significantly improved the enzyme potency. SAR and biological activity of these compounds are presented. The discovery and synthesis of 3-(1 H-benzo dimidazol-2-yl)pyridin-2(1 H)-one inhibitors of insulin-like growth factor 1-receptor (IGF-1R) are presented. Installing amine containing side chains at the 4-position of pyridone ring significantly improved the enzyme potency. SAR and biological activity of these compounds is presented.
