- Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.
Bioorganic & medicinal chemistry letters (2016-07-28)
Haixia Wang, J David Lawson, Nick Scorah, Ruhi Kamran, Mark S Hixon, Joy Atienza, Douglas R Dougan, Mark Sabat
PMID27460209
ZUSAMMENFASSUNG
Using SBDD, a series of 4-amino-7-azaindoles were discovered as a novel class of Alk5 inhibitors that are potent in both Alk5 enzymatic and cellular assays. Subsequently a ring cyclization strategy was utilized to improve ADME properties leading to the discovery of a series of 1H-imidazo[4,5-c]pyridin-2(3H)-one drug like Alk5 inhibitors.
MATERIALIEN