Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor

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• 作者：Lyamin Z. Bendjeddou^a ; ^b ; Nadè ; ge Loaë ; c^a ; Beno&icirc ; t Villiers^a ; Eric Prina^c ; Gerald F. Spä ; th^c ; Hervé ; Galons^b ; Laurent Meijer^a ; ^{meijer@manros-therapeutics.com} ; Nassima Oumata^a ; ^{oumata@manros-therapeutics.com}
• 关键词：Kinase inhibitor ; Imidazo[1 ; 2-b]pyridazine ; Unicellular parasites ; Leishmania ; DYRK1A ; CLKs
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：696-709
• 全文大小：1960 K
• 卷排序：125

文摘

A large variety of imidazo[1,2-b]pyridazines were prepared. The prepared compounds were assayed against a panel of mammalian and protozoan kinases. Several molecules were found to be selective DYRK and CLK inhibitors. Despite their potencies against the kinases studied, the compounds were not cytotoxic.