title: Oxidative regioselective amination of chromones exposes potent inhibitors of the hedgehog signaling pathway.
abstract: A transition metal-free, oxidative, regioselective cross-coupling between non-functionalized azoles and chromones at C2-position was developed. A broad reaction scope and further transformation of products were demonstrated. The biological evaluation of products revealed a novel class of hedgehog signaling pathway inhibitors.
authors.affiliation: Max-Planck Institute of Molecular Physiology, Abteilumg Chemische Biologie, Otto-Hahn Strasse 11, 44227, Dortmund, Germany. andrey.antonchick@mpi-dortmund.mpg.de.
authors.forename: Rajarshi
authors.initials: R
authors.lastname: Samanta
authors.forename: Rishikesh
authors.initials: R
authors.lastname: Narayan
authors.forename: Jonathan O
authors.initials: JO
authors.lastname: Bauer
authors.forename: Carsten
authors.initials: C
authors.lastname: Strohmann
authors.forename: Sonja
authors.initials: S
authors.lastname: Sievers
authors.forename: Andrey P
authors.initials: AP
authors.lastname: Antonchick
mesh_terms: D045744:Cell Line, Tumor; D002867:Chromones / Q000737:chemistry* / Q000494:pharmacology*; D053823:Hedgehog Proteins / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D010084:Oxidation-Reduction; D010847:Picolines; D015398:Signal Transduction / Q000187:drug effects*; D013379:Substrate Specificity
chemical_list: D002867:Chromones; D053823:Hedgehog Proteins; D010847:Picolines; C015672:2-amino-4-picoline