Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.
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Rachid Z, Macphee M, Williams C, Todorova M, Jean-Claude BJ
Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5505-9. doi: 10.1016/j.bmcl.2009.05.060. Epub 2009 May 20.
- PubMed ID
- 19665377 [ View in PubMed]
- Abstract
The monoalkyltriazene moiety lends itself well to the design of combi-molecules. However, due to its instability under physiological conditions, efforts were directed towards stabilizing it by grafting a hydrolysable carbamate onto the 3-position. The synthesis and biological activities of these novel N-carbamyl triazenes are described.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Gefitinib Epidermal growth factor receptor IC 50 (nM) 33 N/A N/A Details