Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands

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• 作者：Miroslav Murá ; r^a ; Juraj Dobia&scaron ; ^a ; Peter &Scaron ; ramel^a ; ^c ; Gabriela Addová ; ^b ; Gilles Hanquet^c ; Andrej Bohá ; č^a ; ^d ; ^{andrej.bohac@fns.uniba.sk}
• 关键词：Dual CLK1/VEGFR2 kinase ligands ; CDK9 ; GSK3 ; DYRK1A ; GSK3α/β ; Muti-targeted kinase inhibitors
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：754-761
• 全文大小：1446 K
• 卷排序：126

文摘

Four novel N-aryloxazol-2-amine CLK1 inhibitors (20,30,40,80 nM) were discovered. Their binding poses in CLK1 and 3 were predicted. Analysis of all CLK PDB structures and interactions of their ligands were performed. An advantageous dual VEGFR2/CLK activity of N-aryloxazol-2-amines was proposed.