Journal of Medicinal Chemistry p. 999 - 1001 (2002)
Update date:2022-07-30
Topics:
Callahan, James F.
Burgess, Joelle L.
Fornwald, James A.
Gaster, Laramie M.
Harling, John D.
Harrington, Frank P.
Heer, Jag
Kwon, Chet
Lehr, Ruth
Mathur
Olson, Barbara A.
Weinstock, Joseph
Laping, Nicholas J.
Screening of our internal compound collection for inhibitors of the transforming growth factor β1 (TGF-β1) 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-β1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay.
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