Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592549 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
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.
Related Topics
Physical Sciences and Engineering
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Authors
Fabrice Pierre, Collin F. Regan, Marie-Claire Chevrel, Adam Siddiqui-Jain, Diwata Macalino, Nicole Streiner, Denis Drygin, Mustapha Haddach, Sean E. O'Brien, William G. Rice, David M. Ryckman,