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

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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