Naphthoquinone compounds are investigated as potential anti-cancer agents due to their ability to generate reactive oxygen species (ROS) and bind to DNA, mechanisms associated with cancer progression. In this study, we tested a series of 1,4-naphthoquinone derivatives in a human breast cancer (BT5) cell line. BT5 cells exhibit elevated LAT1 transporter expression, linked to cancer cells' altered nutrient needs. Two compounds were conjugated to the amino acid tyrosine, an LAT1 substrate, to facilitate selective drug uptake. Cell viability was assessed 48 hours post-treatment using an MTS assay, and IC50 values were calculated to determine potency. Results showed a significant reduction in cell viability in treated groups, consistent with cytotoxic effects reported in other cancer cell lines. These findings highlight the anti-cancer potential of naphthoquinones, particularly in targeting LAT1-mediated drug uptake, and pave the way for future studies on their molecular mechanisms.