4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 14, Pages 4599-4604

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.098

Keywords

PIM kinases; Hit-to-lead; Small molecule inhibitor; Thiazolidine-2,4-dione; X-ray crystallography; Cancer

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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. (C) 2012 Published by Elsevier Ltd.

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