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Issue 11, 2016
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Discovery of dually acting small-molecule inhibitors of cancer-resistance relevant receptor tyrosine kinases EGFR and IGF-1R

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Abstract

Novel benzo-anellated furo- and pyrrolo[2,3-b]pyridines with a 4-benzylamine substitution have been evaluated as inhibitors of the epidermal growth factor receptor (EGFR). Substituent effects on the determined protein kinase affinity have been discussed based on varied benzylamine residues at the differently substituted molecular scaffolds. Docking studies were carried out in order to explore the potential binding modes of the novel inhibitors. The observed activity data encouraged the measurement of the inhibition of the insulin-like growth factor receptor (IGF-1R), which is known to play an important role in the cancer-resistance development against EGFR inhibitors via receptor heterodimerizations with IGF-1R. We identified novel dual inhibitors of both kinases and report their first cancer cell growth inhibition data.

Graphical abstract: Discovery of dually acting small-molecule inhibitors of cancer-resistance relevant receptor tyrosine kinases EGFR and IGF-1R

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Publication details

The article was received on 14 Jun 2016, accepted on 02 Aug 2016 and first published on 09 Sep 2016


Article type: Research Article
DOI: 10.1039/C6MD00329J
Citation: Med. Chem. Commun., 2016,7, 2159-2166
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    Discovery of dually acting small-molecule inhibitors of cancer-resistance relevant receptor tyrosine kinases EGFR and IGF-1R

    C. Hempel, A. Najjar, F. Totzke, C. Schächtele, W. Sippl, C. Ritter and A. Hilgeroth, Med. Chem. Commun., 2016, 7, 2159
    DOI: 10.1039/C6MD00329J

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