JANDELEIT, BERND,FISCHER, WOLF-NICOLAS,KOLLER, KERRY, J.
申请号：
SG11201606351V
公开号：
SG11201606351VA
申请日:
2015.02.03
申请国别(地区):
SG
年份:
2016
代理人:
摘要：
&bgr-Substituted &bgr-amino acids, &bgr-substituted &bgr-amino acid derivatives, and &bgr-substituted &bgr-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The &bgr-substituted &bgr-amino acid derivatives and &bgr-substituted &bgr-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 &bgr-substituted &bgr-amino acid derivatives and &bgr-substituted &bgr-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The &bgr-substituted &bgr-amino acid derivatives and &bgr-substituted &bgr-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 &bgr-substituted &bgr-amino acid derivatives and &bgr-substituted &bgr-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
