Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.

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Boschelli DH, Ye F, Wu B, Wang YD, Barrios Sosa AC, Yaczko D, Powell D, Golas JM, Lucas J, Boschelli F

Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3797-800.

PubMed ID
14552782 [ View in PubMed
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Abstract

Several 7-alkoxy-4-anilino-3-quinolinecarbonitriles were synthesized and evaluated for Src kinase inhibitory activity. Optimal inhibition of both Src enzymatic and cellular activity was seen with analogues having a 2,4-dichloro-5-methoxyaniline group at C-4. Compound 18, which has a 1-methylpiperidinemethoxy group at C-7, showed in vivo activity in a xenograft model.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BosutinibProto-oncogene tyrosine-protein kinase SrcIC 50 (nM)1.27.530Details