Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof
AssigneeQuadriga Biosciences, Inc.
InventorsBernd Jandeleit, Wolf-Nicolas Fischer, Kerry J. Koller, Gordon Ringold
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AssigneeQuadriga Biosciences, Inc.
InventorsBernd Jandeleit, Wolf-Nicolas Fischer, Kerry J. Koller, Gordon Ringold
Estimating the term…
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.
A compound of Formula (1):
The compound (3S)-3-amino-4-[2-[bis(2-chloroethyl)amino]phenyl]butanoic acid or a pharmaceutically acceptable salt thereof.
The compound (3S)-3-amino-4-[2,5-bis[bis(2-chloroethyl)amino]phenyl]butanoic or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.