SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
摘要:
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. (C) 2010 Elsevier Ltd. All rights reserved.
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
摘要:
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. (C) 2010 Elsevier Ltd. All rights reserved.