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US 6,747,009 B2Granted
Peptidomimetic glutathione analogs
AssigneeUniversiteit Leiden
InventorsDanny Burg, Gerard Johan Mulder
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Abstract
The invention relates to peptidomimetic compounds with formula wherein Z═CH2 and Y═CH2, or Z═O and Y═O═O, which are novel analogs of glutathion and are inhibitors of glutathione S-transferase, in particular of GST P1-1. Such inhibition has beneficial effects in therapy against cancer. In particular compounds in which R3 is H, R4 is benzyl and R5 is phenyl are stable towards γGT activity and are selective for GST P1-1.
Claims8
A compound of formula
- wherein
- Z═CH2 and Y═CH2, or
- Z═O and Y═CO═O,
- R1 and R2 are independently selected from the group consisting of H, linear or branched alkyl (1-25C), aralkyl (6-26C), cycloalkyl (6-25C). heterocycles (6-20C), and ethers or polyethers (3-25C), or R1-R2 together have 2-20C atoms and form a macrocycle with the remainder of formula I;
- R3 is selected from the group consisting of H and CH3,
- R1 is selected from the group consisting of 6-8C alkyl, benzyl, naphthyl and a therapeutically active compound, and
- R5 is selected from the group consisting of H, phenyl, Ch3 and CH2phenyl or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.