JANDELEIT BERND,FISCHER WOLF NICOLAS,KOLLER KERRY J
申请号：
IN201637030186
公开号：
IN201637030186A
申请日:
2016.09.03
申请国别(地区):
IN
年份:
2016
代理人:
摘要：
ß Substituted amino acids ß substituted amino acid derivatives and ß substituted amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ß substituted amino acid derivatives and ß substituted amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates capable of passing through the bloodbrain barrier and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the ß substituted amino acid derivatives and ß substituted amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The ß substituted amino acid derivatives and ß substituted amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The ß substituted amino acid derivatives and ß substituted amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
