A novel non-sulphamoylated 2-methoxyestradiol derivative causes detachment of breast cancer cells by rapid disassembly of focal adhesions.

We show that a novel 2ME2 derivative, EE-15-one, induces rapid loss of focal adhesion function leading to cell-substrate detachment through interference with integrin-based cell-substrate adhesions, but not cadherin dependent cell-cell adhesions. Therefore, EE-15-one is the first 2ME2 derivative that has an alternative mode of action to the antimitotic activity of 2ME2. As such EE-15-one shows potential as a lead compound for further development as an inhibitor of cell-substrate adhesion which is essential for metastatic dissemination.