Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
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Nishii H, Chiba T, Morikami K, Fukami TA, Sakamoto H, Ko K, Koyano H
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1405-9. doi: 10.1016/j.bmcl.2009.12.109. Epub 2010 Jan 4.
- PubMed ID
- 20093027 [ View in PubMed]
- Abstract
A novel quinoline derivative that selectively inhibits c-Met kinase was identified. The molecular design is based on a result of the analysis of a PF-2341066 (1)/c-Met cocrystal structure (PDB code: 2wgj). The kinase selectivity of the derivatives is discussed from the view point of the sequence homology of the kinases, the key interactions found in X-ray cocrystal structures, and the structure-activity relationship (SAR) obtained in this work.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Crizotinib Hepatocyte growth factor receptor IC 50 (nM) 8 N/A N/A Details