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Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells

  作者 Pierre, F; Regan, CF; Chevrel, MC; Siddiqui-Jain, A; Macalino, D; Streiner, N; Drygin, D; Haddach, M; O'Brien, SE; Rice, WG; Ryckman, DM  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-9;  页码  3327-3331  
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[摘要]A novel family of potent dual inhibitors of CK2 and the Pim kinases was discovered by modifying the scaffolds of tricyclic Pim inhibitors. Several analogs were active at single digit nanomolar IC50 values against CK2 and the Pim isoforms Pim-1 and Pim-2. The molecules displayed antiproliferative activity in various cell phenotypes in the low micromolar and submicromolar range, providing an excellent starting point for further drug discovery optimization. (C) 2012 Elsevier Ltd. All rights reserved.

 
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