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Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors

…, MJ Romanowski, RA Elling, W Lew, HE Purkey…

文献索引:Hanan, Emily J.; Fucini, Raymond V.; Romanowski, Michael J.; Elling, Robert A.; Lew, Willard; Purkey, Hans E.; VanderPorten, Erica C.; Yang, Wenjin Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5186 - 5189

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被引用次数: 15

摘要

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.