Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series which exhibited potent, picomolar RSK2 inhibition and the most potent in vitro target modulation seen thus far for a RSK inhibitor. In the context of the more potent core, several changes at the phenol moiety were assessed to potentially find a tool molecule appropriate for in vivo evaluation.

中文翻译：

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有效的RSK抑制剂的设计与合成

以已经描述的3,4-双芳基吡啶系列为起点，将第二个环系统与氢键供体和其他疏水性接触结合，得到氮杂吲哚系列，该类氮杂吲哚系列表现出有效的皮摩尔RSK2抑制作用，并且在体外作用最强到目前为止，对于RSK抑制剂的目标调节作用。在更有效的核心的背景下，评估了酚部分的几处变化，以潜在地找到适合体内评估的工具分子。