Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type 1 Receptor (ALK5)
Journal of Medicinal Chemistry2002Vol. 45(5), pp. 999–1001
Citations Over TimeTop 10% of 2002 papers
James F. Callahan, Joelle L. Burgess, James A. Fornwald, Laramie M. Gaster, John D. Harling, Frank P. Harrington, Jag Heer, Chet Kwon, Ruth Lehr, Anil Mathur, Barbara A. Olson, Joseph Weinstock, Nicholas J. Laping
Abstract
Screening of our internal compound collection for inhibitors of the transforming growth factor beta1 (TGF-beta1) type I receptor (ALK5) identified several hits. Optimization of the dihydropyrroloimidazole hit 2 by introduction of a 2-pyridine and 3,4-methylenedioxyphenyl group gave 7, a selective ALK5 inhibitor. With this information, optimization of the triarylimidazole hit 8 gave the selective inhibitor 14, which inhibits TGF-beta1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay.
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