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

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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-07, Vol.22 (14), p.4599-4604
Main 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
Format: Article
Language:English
Subjects:
Animals
Benzylidene Compounds - chemistry
Benzylidene Compounds - pharmacology
Biological and medical sciences
Cancer
Cell Line
Cell Proliferation - drug effects
chemistry
Drug Discovery
Hit-to-lead
Humans
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
PIM kinases
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
protein kinases
Protein-Serine-Threonine Kinases - antagonists & inhibitors
Proto-Oncogene Proteins - antagonists & inhibitors
Rats
Small molecule inhibitor
Structure-Activity Relationship
Thiazolidine-2,4-dione
Thiazolidinediones - chemistry
Thiazolidinediones - pharmacology
X-ray crystallography
X-ray diffraction
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.05.098