301836-29-3

Upstream product

• 301836-28-2 2-(4-cyanophenyl)-4-(4-fluorophenyl)-N-1-hydroxy-5-(2-pyridyl)-imidazole 
• 116332-54-8 4-fluoro-N-methoxy-N-methylbenzamide 
• 366-62-1 2-(4-fluoro-phenyl)-1-pyridin-2-yl-ethanone 

Downstream Products

• 152121-32-9 4-[4-(4-Fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]benzoic acid 
• 301836-30-6 4-[4-(4-Fluorophenyl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzoic acid 

Relevant academic research and scientific papers

Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5)

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

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.