| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363384 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
The SAR of PXR transactivation by 3-(benzimidazol-2-yl)-pyridine-2-one based ATP competitive inhibitors of Insulin-like Growth Factor 1 Receptor kinase (IGF-1R) is discussed. Compounds without PXR transactivation, with in vivo antitumor activity, reduced protein binding and improved oral exposure are presented.
Graphical abstractThe SAR of PXR transactivation by 3-(benzimidazol-2-yl)-pyridine-2-one based ATP competitive inhibitors of Insulin-like Growth Factor 1 Receptor kinase (IGF-1R) is discussed. Compounds without PXR transactivation, with in vivo antitumor activity, reduced protein binding and improved oral exposure are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Kurt Zimmermann, Mark D. Wittman, Mark G. Saulnier, Upender Velaparthi, Xiaopeng Sang, David B. Frennesson, Charles Struzynski, Steven P. Seitz, Liqi He, Joan M. Carboni, Aixin Li, Ann F. Greer, Marco Gottardis, Ricardo M. Attar, Zheng Yang,