β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-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 β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-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 β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.本發明揭示經β-取代的β-胺基酸、經β-取代的β-胺基酸衍生物、及經β-取代的β-胺基酸類似物與(生物)電子等排體和其充當化學治療劑之用途。該經β-取代的β-胺基酸衍生物與經β-取代的β-胺基酸類似物及(生物)電子等排體是選擇性LAT1/4F2hc受質與顯出在表現LAT1/4F2hc運輸蛋白之腫瘤中的迅速吸收與滯留。本發明還揭示合成該經β-取代的β-胺基酸衍生物與經β-取代的β-胺基酸類似物的方法和用該化合物治療癌症的方法。當被體內投予患者時,該經β-取代的β-胺基酸衍生物與經β-取代的β-胺基酸類似物顯出在表現LAT1/4F2hc運輸蛋白之腫瘤細胞中的選擇性吸收與蓄積於癌細胞中。該經β-取代的β-胺基酸衍生物與經β-取代的β-胺基酸類似物和(生物)電子等排體對幾種癌類型顯出細胞毒性。
