Peptidomimetic glutathione analogs

Peptidomimetic glutathione analogs

The invention relates to peptidomimetic compounds with formulawherein 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 c...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: MULDER GERARD JOHAN, BURG DANNY
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:The invention relates to peptidomimetic compounds with formulawherein 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 gammaGT activity and are selective for GST P1-1.