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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) |
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| Authors: | 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 |
| Affiliation: | Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. upender.velaparthi@bms.com |
| Abstract: | The discovery and synthesis of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-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. |
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