2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.

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Determann R, Dreher J, Baumann K, Preu L, Jones PG, Totzke F, Schachtele C, Kubbutat MH, Kunick C

2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.

Eur J Med Chem. 2012 Jul;53:254-63. doi: 10.1016/j.ejmech.2012.04.007. Epub 2012 Apr 14.

PubMed ID

22560627 [ View in PubMed

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Abstract

2-Anilino-4-(benzimidazol-2-yl)-pyrimidines, synthesized by reaction of a readily available benzimidazole-substituted enaminone with suitable arylguanidines, were shown to inhibit four cancer-related protein kinases (Aurora B, PLK1, FAK, and VEGF-R2). The most potent derivative exhibited antiproliferative activity for several cancer cell lines of the NCI in vitro cell line panel in submicromolar concentrations. Both the anilinopyrimidine structure and the substitution pattern at the aniline ring appear to be important for the protein kinase inhibitory activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sunitinib	Vascular endothelial growth factor receptor 2	IC 50 (nM)	70	N/A	N/A	Details