具有改善溶解度和降低蛋白结合能力的高效polo样激酶1噻吩抑制剂的设计
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.
作者信息
Emmitte Kyle A, Adjabeng George M, Andrews C Webb, Alberti Jennifer G Badiang, Bambal Ramesh, Chamberlain Stanley D, Davis-Ward Ronda G, Dickson Hamilton D, Hassler Daniel F, Hornberger Keith R, Jackson Jeffrey R, Kuntz Kevin W, Lansing Timothy J, Mook Robert A, Nailor Kristen E, Pobanz Mark A, Smith Stephon C, Sung Chiu-Mei, Cheung Mui
机构信息
Five Moore Drive, Research Triangle Park, NC 27709, GlaxoSmithKline, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694-7. doi: 10.1016/j.bmcl.2009.01.094. Epub 2009 Jan 31.
A series of thiophene PLK1 inhibitors was optimized for increased solubility and reduced protein binding through the appendage of basic amine functionality. Interesting selectivity between PLK1 and PLK3 was also obtained through these modifications.
通过连接碱性胺官能团，对一系列噻吩类PLK1抑制剂进行了优化，以提高其溶解度并降低蛋白结合率。通过这些修饰，还获得了PLK1和PLK3之间有趣的选择性。
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