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Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
- Source :
- Molecules; Volume 17; Issue 6; Pages: 6317-6330, Molecules
- Publication Year :
- 2012
- Publisher :
- Molecular Diversity Preservation International, 2012.
-
Abstract
- A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase.
- Subjects :
- Sorafenib
Stereochemistry
Protein Conformation
Aurora B kinase
Pharmaceutical Science
Antineoplastic Agents
Plasma protein binding
Molecular Dynamics Simulation
Protein Serine-Threonine Kinases
Article
Analytical Chemistry
Inhibitory Concentration 50
Protein structure
Aurora Kinases
Cell Line, Tumor
Drug Discovery
medicine
N-methylpicolinamide-4-thiol derivatives
Aurora Kinase B
Humans
Sulfhydryl Compounds
Physical and Theoretical Chemistry
Picolinic Acids
Protein Kinase Inhibitors
antitumor
Cell Proliferation
Aurora-B kinase
docking study
Chemistry
Kinase
Organic Chemistry
In vitro
Biochemistry
Chemistry (miscellaneous)
Cell culture
Molecular Medicine
medicine.drug
Protein Binding
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Database :
- OpenAIRE
- Journal :
- Molecules; Volume 17; Issue 6; Pages: 6317-6330
- Accession number :
- edsair.doi.dedup.....8e147356d7578ff6df674e9f7387219f
- Full Text :
- https://doi.org/10.3390/molecules17066317