4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors.
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Zhang N, Wu B, Boschelli DH, Golas JM, Boschelli F
4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5071-4. doi: 10.1016/j.bmcl.2009.07.043. Epub 2009 Jul 10.
- PubMed ID
- 19632113 [ View in PubMed]
- Abstract
A series of 4-anilino-7-pyridyl-3-quinolinecarbonitriles was prepared as Src kinase inhibitors. A systematic SAR study of substitutions on both the pyridine ring and the 3-quinolinecarbonitrile core established the requirements for optimal activity. The lead compound, 17, showed potent activity in both the Src enzyme assay and cell assays, and demonstrated in vivo anti-tumor activity in a xenograft model.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bosutinib Proto-oncogene tyrosine-protein kinase Src IC 50 (nM) 100 N/A N/A Details Bosutinib Proto-oncogene tyrosine-protein kinase Src IC 50 (nM) 3.8 N/A N/A Details