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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.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Jul 15; Vol. 22 (14), pp. 4599-604. Date of Electronic Publication: 2012 Jun 06. - Publication Year :
- 2012
-
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.<br /> (Copyright © 2012. Published by Elsevier Ltd.)
- Subjects :
- Animals
Benzylidene Compounds pharmacology
Cell Line
Cell Proliferation drug effects
Drug Discovery
Humans
Models, Molecular
Protein Kinase Inhibitors pharmacology
Rats
Structure-Activity Relationship
Thiazolidinediones pharmacology
Benzylidene Compounds chemistry
Protein Kinase Inhibitors chemistry
Protein Serine-Threonine Kinases antagonists & inhibitors
Proto-Oncogene Proteins antagonists & inhibitors
Thiazolidinediones chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22727640
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.05.098