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BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
专利权人:
QUADRIGA BIOSCIENCES; INC.
发明人:
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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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