Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.

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Boschelli DH, Wang D, Wang Y, Wu B, Honores EE, Barrios Sosa AC, Chaudhary I, Golas J, Lucas J, Boschelli F

Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.

Bioorg Med Chem Lett. 2010 May 1;20(9):2924-7. doi: 10.1016/j.bmcl.2010.03.025. Epub 2010 Mar 7.

PubMed ID

20363128 [ View in PubMed

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Abstract

The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC(50) values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.

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