| NĚMEC, Václav, Lukáš MAIER, Benedict-Tilman BERGER, Apirat CHAIKUAD, Stanislav DRÁPELA, Karel SOUČEK, Stefan KNAPP and Kamil PARUCH. Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. European Journal of Medicinal Chemistry. Elsevier Masson s.r.l., 2021, vol. 215, April, p. "113299", 8 pp. ISSN 0223-5234. Available from: https://dx.doi.org/10.1016/j.ejmech.2021.113299. |
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@article{1764607,
author = {Němec, Václav and Maier, Lukáš and Berger, BenedictandTilman and Chaikuad, Apirat and Drápela, Stanislav and Souček, Karel and Knapp, Stefan and Paruch, Kamil},
article_number = {April},
doi = {http://dx.doi.org/10.1016/j.ejmech.2021.113299},
keywords = {Kinase; Inhibitor; Furo[3.2-b]pyridine; HIPK; MU135; MU1787; CLK; MU1210},
language = {eng},
issn = {0223-5234},
journal = {European Journal of Medicinal Chemistry},
title = {Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core},
url = {https://doi.org/10.1016/j.ejmech.2021.113299},
volume = {215},
year = {2021}
}
TY - JOUR
ID - 1764607
AU - Němec, Václav - Maier, Lukáš - Berger, Benedict-Tilman - Chaikuad, Apirat - Drápela, Stanislav - Souček, Karel - Knapp, Stefan - Paruch, Kamil
PY - 2021
TI - Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core
JF - European Journal of Medicinal Chemistry
VL - 215
IS - April
SP - "113299"
EP - "113299"
PB - Elsevier Masson s.r.l.
SN - 02235234
KW - Kinase
KW - Inhibitor
KW - Furo[3.2-b]pyridine
KW - HIPK
KW - MU135
KW - MU1787
KW - CLK
KW - MU1210
UR - https://doi.org/10.1016/j.ejmech.2021.113299
N2 - The furo [3,2-b]pyridine motif represents a relatively underexplored central pharmacophore in the area of kinase inhibitors. Herein, we report flexible synthesis of 3,5-disubstituted furo [3,2-b]pyridines that relies on chemoselective couplings of newly prepared 5-chloro-3-iodofuro [3,2-b]pyridine. This methodology allowed efficient second-generation synthesis of the state-of-the-art chemical biology probe for CLK1/2/4 MU1210, and identification of the highly selective inhibitors of HIPKs MU135 and MU1787 which are presented and characterized in this study, including the X-ray crystal structure of MU135 in HIPK2. chemical biology probe (c) 2021 Published by Elsevier Masson SAS.
ER -
NĚMEC, Václav, Lukáš MAIER, Benedict-Tilman BERGER, Apirat CHAIKUAD, Stanislav DRÁPELA, Karel SOUČEK, Stefan KNAPP and Kamil PARUCH. Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. \textit{European Journal of Medicinal Chemistry}. Elsevier Masson s.r.l., 2021, vol.~215, April, p.~''113299'', 8 pp. ISSN~0223-5234. Available from: https://dx.doi.org/10.1016/j.ejmech.2021.113299.
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