| Literature DB >> 22460033 |
Fabrice Pierre1, 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.
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 IC(50) 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.Entities:
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Year: 2012 PMID： 22460033 DOI： 10.1016/j.bmcl.2012.02.099
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823