301836-28-2Relevant academic research and scientific papers
Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5)
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.
, p. 999 - 1001 (2007/10/03)
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.
Triarylimidazoles
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, (2008/06/13)
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2and R3are various substituent groups; and one of X1and X2is N or CR′, and the other is NR′ or CHR′ wherein R′ is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1and X2is N or CR′ then the other may be S or O; and their use as pharmaceuticals.
