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