Chemical Sciences, Pfizer Global Research and Development, Collegeville, PA 19335, USA.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3821-5. doi: 10.1016/j.bmcl.2010.04.022. Epub 2010 Apr 18.
A series of tricyclic anilinopyrimidines were synthesized and evaluated as IKKbeta inhibitors. Several analogues, including tricyclic phenyl (10, 18a, 18c, 18d, and 18j) and thienyl (26 and 28) derivatives were shown to have good in vitro enzyme potency and excellent cellular activity. Pharmaceutical profiling of a select group of tricyclic compounds compared to the non-tricyclic analogues suggested that in some cases, the improved cellular activity may be due to increased clog P and permeability.
合成了一系列三环苯胺嘧啶并对其进行了 IKKβ 抑制活性评价。部分类似物如三环苯（10、18a、18c、18d 和 18j）和噻吩（26 和 28）衍生物表现出良好的体外酶活性和优异的细胞活性。对一组三环化合物和非三环类似物的药物特性分析表明，在某些情况下，细胞活性的提高可能是由于 clog P 和通透性的增加。
Zotero 插件