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. 2010 Mar 1;20(5):1744-8.
doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21.

SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors

Kurt Zimmermann  1 , 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, Praveen Balimane, Lorell N Discenza, Francis Y Lee, Michael Sinz, Sean Kim, Dolatrai Vyas
Affiliations

SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors

Kurt Zimmermann et al. Bioorg Med Chem Lett. .

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.

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