[beta]-Substituted [beta]-amino acids, [beta]-substituted [beta]-amino acid derivatives, and [beta]-substituted [beta]-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The [beta]-substituted [beta]-amino acid derivatives and [beta]-substituted [beta]-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the [beta]-substituted [beta]-amino acid derivatives and [beta]-substituted [beta]-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The [beta]-substituted [beta]-amino acid derivatives and [beta]-substituted [beta]-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The [beta]-substituted [beta]-amino acid derivatives and [beta]-substituted [beta]-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.本發明提供一種β-取代的β-胺基酸、β-取代的β-胺基酸衍生物、β-取代的β-胺基酸類似物及(生物)電子等排體及其作為化療劑的用途。所述β-取代的β-胺基酸衍生物、β-取代的β-胺基酸類似物及(生物)電子等排體係選擇性LAT1/4F2hc受質，並在表現LAT1/4F2hc運輸蛋白的腫瘤中顯示快速吸收及保留。亦提供合成所述β-取代的β-胺基酸衍生物及β-取代的β-胺基酸類似物的方法，以及使用所述化合物治療治療惡性腫瘤的方法。當在體內施用於對象時，所述β-取代的β-胺基酸衍生物及β-取代的β-胺基酸類似物在表現LAT1/4F2hc運輸蛋白的腫瘤細胞中顯示選擇性吸收，並在惡性腫瘤細胞內累積。所述β-取代的β-胺基酸衍生物、β-取代的β-胺基酸類似物及(生物)電子等排體對多種腫瘤類型顯示細胞毒性。
