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Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2014 Jun 10; Vol. 80, pp. 364-82. Date of Electronic Publication: 2014 Apr 05. - Publication Year :
- 2014
-
Abstract
- The Cell division cycle 7 (Cdc7) protein kinase is essential for DNA replication and maintenance of genome stability. We systematically explored thiazole-based compounds as inhibitors of Cdc7 kinase activity in cancer cells. Our studies resulted in the identification of a potent, selective Cdc7 inhibitor that decreased phosphorylation of the direct substrate MCM2 in vitro and in vivo, and inhibited DNA synthesis and cell viability in vitro.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Catalytic Domain
Cell Cycle Proteins chemistry
Cell Cycle Proteins metabolism
Cell Line, Tumor
Chemistry Techniques, Synthetic
Female
HCT116 Cells
Humans
Inhibitory Concentration 50
Male
Mice
Minichromosome Maintenance Complex Component 2 metabolism
Molecular Docking Simulation
Phosphorylation drug effects
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors metabolism
Protein Serine-Threonine Kinases chemistry
Protein Serine-Threonine Kinases metabolism
Rats
Structure-Activity Relationship
Thiazoles chemistry
Thiazoles metabolism
Xenograft Model Antitumor Assays
Cell Cycle Proteins antagonists & inhibitors
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Protein Serine-Threonine Kinases antagonists & inhibitors
Thiazoles chemical synthesis
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 80
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 24793884
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.04.013