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.
Zakaria Rachid  1 ,  Meaghan Macphee ,  Christopher Williams ,  Margarita Todorova ,  Bertrand Jacques Jean-Claude
Affiliations
  • 1. Cancer Drug Research Laboratory, Division of Medical Oncology, Department of Medicine, McGill University/Royal Victoria Hospital, 687 Pine Avenue west Rm M-719, Montreal, Québec, Canada H3A 1A1.
PMID: 19665377 DOI: 10.1016/j.bmcl.2009.05.060
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.