| abstract |
Disclosed are β-substituted β-amino acids, β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs, and (bio) isostars, and their use as chemotherapeutic agents. β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio) isostars are selective LAT1 / 4F2hc substrates and show rapid uptake and retention in tumors expressing the LAT1 / 4F2hc transporter. Also disclosed are methods of synthesizing β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs, and methods of using the compounds to treat cancer. β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs, when administered in vivo to a subject, exhibit selective uptake in tumor cells expressing the LAT1 / 4F2hc transporter and accumulation in cancerous cells. Show. β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio) isostars are cytotoxic to several tumor types. |