作为Polo样激酶抑制剂的2-氨基异恶唑并吡啶的设计与合成
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.
作者信息
Hanan Emily J, Fucini Raymond V, Romanowski Michael J, Elling Robert A, Lew Willard, Purkey Hans E, VanderPorten Erica C, Yang Wenjin
机构信息
Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard Suite 400, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5186-9. doi: 10.1016/j.bmcl.2008.08.091. Epub 2008 Aug 29.
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.
设计并合成了一系列2-氨基异恶唑并吡啶作为Polo样激酶（Plk）抑制剂。讨论了关键的构效关系（SAR）和晶体学数据。更先进的类似物以良好的酶活性和适度的基于细胞的活性抑制Plk1。观察到三种Plk亚型之间的差异选择性。
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