Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure

  • Eur J Med Chem. 2011 Jul;46(7):2759-69. doi: 10.1016/j.ejmech.2011.03.065.
Stefanie Schmidt  1 ,  Lutz Preu ,  Thomas Lemcke ,  Frank Totzke ,  Christoph Schächtele ,  Michael H G Kubbutat ,  Conrad Kunick
Affiliations
  • 1. Technische Universität Braunschweig, Institut für Pharmazeutische Chemie, Beethovenstraße 55, D-38106 Braunschweig, Germany.
PMID: 21524503 DOI: 10.1016/j.ejmech.2011.03.065
Abstract

The N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide motif was identified as a novel scaffold for the development of kinase inhibitors. Derivatives with a biphenyl element attached to the hydrazide structure proved to be submicromolar dual inhibitors of the cancer-related kinases IGF-1R and Src. One of the most potent kinase inhibitors of the series produced a selective growth inhibition in a panel of cultivated Cancer cell lines.

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