1046831-98-4Relevant articles and documents
Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway
Němec, Václav,Hylsová, Michaela,Maier, Luká?,Flegel, Jana,Sievers, Sonja,Ziegler, Slava,Schr?der, Martin,Berger, Benedict-Tilman,Chaikuad, Apirat,Val?íková, Barbora,Uldrijan, Stjepan,Drápela, Stanislav,Sou?ek, Karel,Waldmann, Herbert,Knapp, Stefan,Paruch, Kamil
supporting information, p. 1062 - 1066 (2019/01/04)
Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines revealed sub-micromolar modulators of the Hedgehog pathway.
Substituted Quinolines and Their Use As Medicaments
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Paragraph 0220, (2013/03/26)
Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
