The design and synthesis of a novel series of 2,6-disubstituted pyrazine derivatives as CK2 kinase inhibitors is described. Structure-guided optimization of a 5-substituted-3-thiophene carboxylic acid screening hit (3a) led to the development of a lead compound (12b), which shows inhibition in both enzymatic and cellular assays. Subsequent design and hybridization efforts also led to the unexpected identification of analogs with potent PIM kinase activity (14f).

中文翻译：

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发现2,6-二取代的吡嗪衍生物作为CK2和PIM激酶的抑制剂

描述和设计了一系列新型的2,6-二取代吡嗪衍生物作为CK2激酶抑制剂。对5-取代的3-噻吩羧酸筛选结果（3a）进行结构导向的优化导致了前导化合物（12b）的开发，该化合物在酶促和细胞分析中均表现出抑制作用。随后的设计和杂交努力也导致了具有有效PIM激酶活性的类似物的意外鉴定（14f）。