Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
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- 作者：Emily J. Hanan ; Raymond V. Fucini ; Michael J. Romanowski ; Robert A. Elling ; Willard Lew ; Hans E. Purkey ; Erica C. V ; erPorten ; Wenjin Yang
- 关键词：2-Amino-isoxazolopyridines ; Polo-like kinase (Plk) ; SAR ; Kinase inhibitor
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：1 October 2008
- 年：2008
- 卷：18
- 期：19
- 页码：5186-5189
- 全文大小：326 K
文摘
A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit Plk1 with good enzymatic activity and modest cell-based activity. Differential selectivity among the three Plk isoforms is observed.