Despite advancements in cancer therapies and multidrug resistance, mechanisms continue to challenge existing treatments, highlighting the need for selective, effective, and affordable options. One solution to this is to target cellular pathways or transporters that are overexpressed in most cancer cells. Targeting the L-type Amino Acid Transporter 1 (LAT1) proves to be a promising approach where LAT1 mediates the uptake of essential amino acids like leucine, isoleucine, methionine, valine, phenylalanine, tryptophan, and tyrosine. Naphthoquinone and acridine cores are known for their indiscriminate cytotoxicity. Conjugating those cores with amino acids to create LAT1-compatible derivatives can enhance selectivity for cancer cells while minimizing off-target effects. This research focuses on developing naphthoquinone-tyrosine and acridine-lysine derivatives to achieve LAT1-mediated drug delivery. The presentation will cover (1) the study of pharmacokinetic properties of naphthoquinone derivatives in silico using SwissADME, and (2) the synthetic strategy for making acridine-lysine derivatives as potential LAT1 substrates.