JANDELEIT, BERND,FISCHER, WOLF-NICOLAS,KOLLER, KERRY J.
申请号：
CA2938571
公开号：
CA2938571A1
申请日:
2015.02.03
申请国别(地区):
CA
年份:
2015
代理人:
摘要：
ß-Substituted ß-amino acids, ß-substituted ß-amino acid derivatives, and ß-substituted ß-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ß-substituted ß-amino acid derivatives and ß-substituted ß-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 ß-substituted ß-amino acid derivatives and ß-substituted ß-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ß-substituted ß-amino acid derivatives and ß-substituted ß-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 ß-substituted ß-amino acid derivatives and ß-substituted ß-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
