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.
- MeSH
- furany chemická syntéza metabolismus farmakologie MeSH
- inhibitory proteinkinas chemická syntéza metabolismus farmakologie MeSH
- krystalografie rentgenová MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- molekulární struktura MeSH
- myši MeSH
- protein-serin-threoninkinasy antagonisté a inhibitory metabolismus MeSH
- pyridiny chemická syntéza metabolismus farmakologie MeSH
- transportní proteiny antagonisté a inhibitory metabolismus MeSH
- vazba proteinů MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH