Document Report Card

Basic Information

ID: ALA1155377

Journal: Bioorg Med Chem Lett

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

Authors: Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D.

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.

CiteXplore: 20153189

DOI: 10.1016/j.bmcl.2010.01.087