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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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