Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core
| Authors | |
|---|---|
| Year of publication | 2021 |
| Type | Article in Periodical |
| Magazine / Source | European Journal of Medicinal Chemistry |
| MU Faculty or unit | |
| Citation | |
| 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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