abstract |
Disclosed herein are? -Substituted? -Amino acids,? -Substituted? -Amino acid derivatives, and? -Substituted? -Amino acid analogs and (bio) copper esters, and their use as chemotherapeutic agents. The? -Substituted? -Amino acid derivatives and? -Substituted? -Amino acid analogs and (bio) copper complexes are selective LAT1 / 4F2hc substrates and exhibit rapid aspiration and retention in tumors expressing the LAT1 / 4F2hc transporter. Also disclosed are methods of synthesizing? -Substituted? -Amino acid derivatives and? -Substituted? -Amino acid analogs and methods of using these compounds in the treatment of cancer. The? -Substituted? -Amino acid derivative and? -Substituted? -Amino acid analogue, when administered to an individual in vivo, exhibit selective aspiration in tumor cells expressing the LAT1 / 4F2hc transporter and accumulate cancer cells. The? -Substituted? -Amino acid derivatives and? -Substituted? -Amino acid analogs and (bio) copper coins exhibit cytotoxicity for several tumor types. |