Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors |
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| Authors: | Hanan Emily J Fucini Raymond V Romanowski Michael J Elling Robert A Lew Willard Purkey Hans E VanderPorten Erica C Yang Wenjin |
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| Institution: | Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard Suite 400, South San Francisco, CA 94080, USA. info@sunesis.com |
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| 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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