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

  • Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. doi: 10.1016/j.bmcl.2012.05.098.
Les A Dakin  1 ,  Michael H Block ,  Huawei Chen ,  Erin Code ,  James E Dowling ,  Xiaomei Feng ,  Andrew D Ferguson ,  Isabelle Green ,  Alexander W Hird ,  Tina Howard ,  Erika K Keeton ,  Michelle L Lamb ,  Paul D Lyne ,  Hannah Pollard ,  Jon Read ,  Allan J Wu ,  Tao Zhang ,  Xiaolan Zheng
Affiliations
  • 1. Oncology iMed Sciences Group, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
PMID: 22727640 DOI: 10.1016/j.bmcl.2012.05.098
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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