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Bioorg Med Chem Lett. 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.

Author information

1
Oncology Chemistry, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA. Kurt.Zimmermann@bms.com

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.

PMID:
20153189
DOI:
10.1016/j.bmcl.2010.01.087
[Indexed for MEDLINE]

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