Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2

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.

Graphical abstractThe synthesis and biological activities of stabilized 3-alkyl-1,2,3-triazene-based EGFR-DNA targeting molecules are described.Figure optionsDownload full-size imageDownload as PowerPoint slide