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Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Oct 21; Vol. 12 (20), pp. 2893-7. - Publication Year :
- 2002
-
Abstract
- The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.
- Subjects :
- Cell Line
Cyclization
Magnetic Resonance Spectroscopy
Mass Spectrometry
Models, Molecular
Molecular Conformation
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
ErbB Receptors antagonists & inhibitors
Nitriles chemical synthesis
Nitriles pharmacology
Quinolines chemical synthesis
Quinolines pharmacology
Receptor, ErbB-2 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12270171
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00598-x