Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core

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NĚMEC Václav MAIER Lukáš BERGER Benedict-Tilman CHAIKUAD Apirat DRÁPELA Stanislav SOUČEK Karel KNAPP Stefan PARUCH Kamil

Year of publication 2021
Type Article in Periodical
Magazine / Source European Journal of Medicinal Chemistry
MU Faculty or unit

Faculty of Science

Web https://doi.org/10.1016/j.ejmech.2021.113299
Doi http://dx.doi.org/10.1016/j.ejmech.2021.113299
Keywords Kinase; Inhibitor; Furo[3.2-b]pyridine; HIPK; MU135; MU1787; CLK; MU1210
Description 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.
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