2019
Němec, Václav; Hylsová, Michaela; Maier, Lukáš; Flegel, Jana; Sievers, Sonja; Ziegler, Slava; Schröder, Martin; Berger, Benedict-Tilman; Chaikuad, Apirat; Valčíková, Barbora; Uldrijan, Stjepan; Drápela, Stanislav; Souček, Karel; Waldmann, Herbert; Knapp, Stefan; Paruch, Kamil
Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway. Journal Article
In: Angewandte Chemie (International ed. in English), vol. 58, no. 4, pp. 1062–1066, 2019, ISSN: 1521-3773 1433-7851, (Place: Germany).
Abstract | Links | BibTeX | Tags: Binding Sites, biological activity, Cell Survival/drug effects, chemical probes, Furans/*chemistry, Hedgehog Proteins/*chemistry, heterocycles, Humans, inhibitors, Inhibitory Concentration 50, kinases, MCF-7 Cells, Molecular Structure, Protein Binding, Protein Kinase Inhibitors/*chemical synthesis/chemistry/pharmacology, Pyridines/*chemistry, Small Molecule Libraries/*chemical synthesis/chemistry/pharmacology
@article{nemec_furo32-bpyridine_2019,
title = {Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway.},
author = {Václav Němec and Michaela Hylsová and Lukáš Maier and Jana Flegel and Sonja Sievers and Slava Ziegler and Martin Schröder and Benedict-Tilman Berger and Apirat Chaikuad and Barbora Valčíková and Stjepan Uldrijan and Stanislav Drápela and Karel Souček and Herbert Waldmann and Stefan Knapp and Kamil Paruch},
doi = {10.1002/anie.201810312},
issn = {1521-3773 1433-7851},
year = {2019},
date = {2019-01-01},
journal = {Angewandte Chemie (International ed. in English)},
volume = {58},
number = {4},
pages = {1062–1066},
abstract = {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.},
note = {Place: Germany},
keywords = {Binding Sites, biological activity, Cell Survival/drug effects, chemical probes, Furans/*chemistry, Hedgehog Proteins/*chemistry, heterocycles, Humans, inhibitors, Inhibitory Concentration 50, kinases, MCF-7 Cells, Molecular Structure, Protein Binding, Protein Kinase Inhibitors/*chemical synthesis/chemistry/pharmacology, Pyridines/*chemistry, Small Molecule Libraries/*chemical synthesis/chemistry/pharmacology},
pubstate = {published},
tppubtype = {article}
}