Cancer focused research continues to attract a lot of attention. Challenges with treating the disease are due in part to cancer cells’ capacity to develop resistance to treatment and to type-specific cellular mechanisms that require focused therapies. A promising target in the development of cancer therapeutics is the L-type amino acids transporter 1 (LAT1). LAT1 is overexpressed in most cancers and plays a crucial role in the uptake of essential amino acids needed for growth and proliferation. In an effort to minimize side effects and circumvent the capacity for cancer cells to develop treatment-resistance, this study aims to exploit LAT1 for the selective delivery of therapeutic agents to cancer cells. This work will synthesize prodrugs integrating 1,4-naphthoquinones with known anticancer properties with LAT1-compatible amino acids such as tyrosine, essentially designing amino acid-naphthoquinone derivatives that mimic LAT1 substrates. This approach holds the potential to improve therapeutic outcomes by leveraging LAT1’s role in amino acid transport to target cancers with greater precision. The presentation will discuss current results in the synthetic approach for making the derivatives and the structural characterization of the compounds.