Publication Abstract from PubMed
A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors of glycogen synthase kinase-3beta with the help of ab initio calculations and a docking study. Enzymatic assay and an X-ray complex study showed that these designed compounds were highly potent ATP-competitive inhibitors.
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.,Shin D, Lee SC, Heo YS, Lee WY, Cho YS, Kim YE, Hyun YL, Cho JM, Lee YS, Ro S Bioorg Med Chem Lett. 2007 Oct 15;17(20):5686-9. Epub 2007 Aug 19. PMID:17764934[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.