Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
2-氨基异恶唑吡啶作为 Polo 样激酶抑制剂的设计和合成
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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 VanderPorten, Wenjin Yang
Abstract
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.
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