doi: 10.1016/j.bmcl.2010.01.087.
Epub 2010 Jan 21.
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
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- PMID: 20153189
- DOI: 10.1016/j.bmcl.2010.01.087
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SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
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.
Copyright 2010 Elsevier Ltd. All rights reserved.
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