Publication Abstract from PubMed
Novel bis(indolyl)maleimide pyridinophanes 3, 9a, 9b, 10a, 10b, and 11 were prepared by cobalt-mediated [2+2+2] cycloaddition of an appropriate alpha,omega-diyne with an N,N-dialkylcyanamide. These macrocyclic heterophanes were found to be potent, selective inhibitors of glycogen synthase kinase-3beta. An X-ray structure of a co-crystal of GSK-3beta and 3 (IC(50)=3nM) depicts the hydrogen bonding and hydrophobic interactions in the ATP-binding pocket of this serine/threonine protein kinase.
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.,Zhang HC, Bonaga LV, Ye H, Derian CK, Damiano BP, Maryanoff BE Bioorg Med Chem Lett. 2007 May 15;17(10):2863-8. Epub 2007 Feb 25. PMID:17350261[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
