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4-Anilino-3-cyanobenzo[g]quinolines as Kinase Inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 12:423-425
- Publication Year :
- 2002
- Publisher :
- Elsevier BV, 2002.
-
Abstract
- A series of 4-anilino-3-cyanobenzo[g]quinolines was prepared as potent kinase inhibitors. Compared with their bicyclic 4-anilino-3-cyanoquinoline analogues, the tricyclic 4-anilino-3-cyanobenzo[g]quinolines are less active against EGF-R kinase, equally active against MAPK kinase (MEK), and more active against Src kinase. For Src kinase inhibition, the best activity is obtained when both the 7- and 8-positions are substituted with alkoxy groups. Several of these kinase inhibitors show potent growth inhibitory activity in tumor cells.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Chemical synthesis
Substrate Specificity
Structure-Activity Relationship
Nitriles
Drug Discovery
polycyclic compounds
Enzyme Inhibitors
Protein Kinase Inhibitors
Molecular Biology
Cells, Cultured
chemistry.chemical_classification
Bicyclic molecule
biology
Chemistry
Kinase
Organic Chemistry
ErbB Receptors
src-Family Kinases
Enzyme
Enzyme inhibitor
Mitogen-activated protein kinase
Quinolines
biology.protein
Molecular Medicine
Indicators and Reagents
Mitogen-Activated Protein Kinases
Signal transduction
Cell Division
Proto-oncogene tyrosine-protein kinase Src
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 12
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....92b33f7bbefb015ee2adf8d36cc3a55d