2. Academic Validation
  3. 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines

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.
Renate Determann 1,  Jan Dreher,  Knut Baumann,  Lutz Preu,  Peter G Jones,  Frank Totzke,  Christoph Schächtele,  Michael H G Kubbutat,  Conrad Kunick
Affiliations

Affiliation

  • 1 Technische Universität Braunschweig, Institut für Medizinische und Pharmazeutische Chemie, Beethovenstraße 55, D-38106 Braunschweig, Germany.
PMID: 22560627 DOI: 10.1016/j.ejmech.2012.04.007
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.

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