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@article{1494217,
author = {Němec, Václav and Hylsová, Michaela and Maier, Lukáš and Flegel, Jana and Sievers, Sonja and Ziegler, Slava and Schröder, Martin and Berger, BenedictandTilman and Chaikuad, Apirat and Valčíková, Barbora and Uldrijan, Stjepan and Drápela, Stanislav and Souček, Karel and Waldmann, Hebert and Knapp, Stefan and Paruch, Kamil},
article_location = {Weinheim},
article_number = {4},
doi = {http://dx.doi.org/10.1002/anie.201810312},
keywords = {biological activity; chemical probes; heterocycles; inhibitors; kinases},
language = {eng},
issn = {1433-7851},
journal = {Angewandte Chemie International Edition},
title = {Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway},
url = {https://onlinelibrary.wiley.com/doi/epdf/10.1002/anie.201810312},
volume = {58},
year = {2019}
}
TY - JOUR
ID - 1494217
AU - 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, Hebert - Knapp, Stefan - Paruch, Kamil
PY - 2019
TI - Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway
JF - Angewandte Chemie International Edition
VL - 58
IS - 4
SP - 1062-1066
EP - 1062-1066
PB - Wiley-VCH
SN - 14337851
KW - biological activity
KW - chemical probes
KW - heterocycles
KW - inhibitors
KW - kinases
UR - https://onlinelibrary.wiley.com/doi/epdf/10.1002/anie.201810312
L2 - https://onlinelibrary.wiley.com/doi/epdf/10.1002/anie.201810312
N2 - 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.
ER -
NĚMEC, Václav, Michaela HYLSOVÁ, Lukáš MAIER, Jana FLEGEL, Sonja SIEVERS, Slava ZIEGLER, Martin SCHRÖDER, Benedict-Tilman BERGER, Apirat CHAIKUAD, Barbora VALČÍKOVÁ, Stjepan ULDRIJAN, Stanislav DRÁPELA, Karel SOUČEK, Hebert WALDMANN, Stefan KNAPP a Kamil PARUCH. Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway. \textit{Angewandte Chemie International Edition}. Weinheim: Wiley-VCH, 2019, roč.~58, č.~4, s.~1062-1066. ISSN~1433-7851. Dostupné z: https://dx.doi.org/10.1002/anie.201810312.
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