Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases |
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Authors: | Dakin Les A Block Michael H Chen Huawei Code Erin Dowling James E Feng Xiaomei Ferguson Andrew D Green Isabelle Hird Alexander W Howard Tina Keeton Erika K Lamb Michelle L Lyne Paul D Pollard Hannah Read Jon Wu Allan J Zhang Tao Zheng Xiaolan |
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Institution: | Oncology iMed Sciences Group, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. |
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Abstract: | Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The synthesis and SAR of these compounds are described, along with X-ray crystallographic, anti-proliferative, and selectivity data. |
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