Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R)

Upender Velaparthi,Mark D Wittman,Peiying Liu,Karen M Stoffan,Kurt Zimmermann,Xiaopeng Sang,Joan M Carboni,Aixin Li,Ricardo M Attar,Marco M Gottardis,Ann Greer,ChiehYing Y. Chang, Bruce L. Jacobsen,John S. Sack,Yax Sun,David R. Langley,Balu N Balasubramanian,Dolatrai M Vyas

Bioorganic & Medicinal Chemistry Letters（2007）

Cited 41|Views24

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Abstract

The discovery and synthesis of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-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.

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Key words

Insulin-like growth factor-1 receptor,Tyrosine kinase,Benzimidazole,Pyridone

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