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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