Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor

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• 作者：Barrios Sosa ; Ana Carolina ; Boschelli ; Diane H. ; Wu ; Biqi ; Wang ; Yan ; Golas ; Jennifer M.
• 关键词：Src ; Kinase ; 3-Quinolinecarbonitriles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：March 15, 2005
• 年：2005
• 卷：15
• 期：6
• 页码：1743-1747
• 全文大小：120 K

文摘

Several new ethynyl- and ethenyl-4-phenylamino-3-quinolinecarbonitriles were synthesized and tested for Src inhibition. Derivatives bearing an ethenyl or ethynyl substituent at C-6 showed decreased Src inhibitory activity. Incorporation of an ethenylpyridine N-oxide group at C-7 provided 20b, a 0.6nM inhibitor of Src enzymatic activity with excellent cellular potency.