Pim kinases are promising therapeutic targets for the treatment of hematological cancers. A potent Pim kinase inhibitor 7f, derived from meridianin C, was further optimized by the replacement of 2-aminopyrimidine with substituted benzene. The optimization of the C-3 and C-5 positions of indole yielded compound 43 with improved cellular potency and high selectivity against a panel of 14 different kinases.

中文翻译：

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发现和评估3,5-二取代的吲哚衍生物作为Pim激酶抑制剂

Pim激酶是用于治疗血液系统癌症的有希望的治疗靶标。通过取代苯取代2-氨基嘧啶，进一步优化了源自子午线蛋白C的有效Pim激酶抑制剂7f。吲哚的C-3和C-5位置的最优化产生具有改善的细胞效力和对一组14种不同激酶的高选择性的化合物43。