RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite re-search into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl–pyridine based compounds that have improved cellular activity while maintaining selectivity for RIOK2. While our compounds do not represent RIOK2 chemical probes, they are the best available tool molecules to begin to characterize RIOK2 function in vitro.

中文翻译：

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迈向 RIOK2 化学探针：选择性 2-(酰氨基)吡啶系列的细胞效力提高

RIOK2 是一种尚未被研究的激酶，与多种人类癌症（包括非小细胞肺癌和胶质母细胞瘤）相关。目前不存在针对 RIOK2 的有效、选择性和细胞活性化学探针。这种试剂将加快对 RIOK2 生物学功能的研究，并验证其作为治疗靶点的效果。在此，我们描述了基于萘基-吡啶的化合物的合成，这些化合物改善了细胞活性，同时保持了对 RIOK2 的选择性。虽然我们的化合物不代表 RIOK2 化学探针，但它们是开始在体外表征 RIOK2 功能的最佳可用工具分子。