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The potent N -methyl-d-aspartate (NMDA) receptor antagonists 1 - 3 have been demonstrated to show antiproliferative and cytotoxic effects in MCF-7 and SKBR3 breast cancer cell lines. To improve the knowledge about the role played by the NMDA receptor in the antitumor activity of these compounds, the enantiomers of 1 were prepared and evaluated for their affinity for the phencyclidine (PCP) site of the NMDA receptor and for their cytotoxic effect in MCF-7 and SKBR3 cell lines, both expressing the NMDA receptor. The ( S )- 1 enantiomer, showing negligible affinity for the PCP site, exhibited antiproliferative activity higher than that of ( R )- 1 , which instead bound the PCP site. The downregulation of NMDA GluN1 expression resulted in a decreased ( S )- 1 -induced cytotoxicity and apoptotic cell death, unequivocally demonstrating the involvement of the NMDA receptor in the antitumor effect of this compound. Due to its interesting biological profile, ( S )- 1 represents a lead compound to develop novel antitumor agents for breast cancer treatment.

Role of the NMDA Receptor in the Antitumor Activity of Chiral 1,4-Dioxane Ligands in MCF-7 and SKBR3 Breast Cancer Cells