Mimetic peptides and the use thereof in the form of 20S, 26S and immunoproteasome inhibitors

摘要

The present invention relates to peptide-mimetic compounds, the synthesis and use thereof fort he inhibition of proteasomes and the induction of apoptosis in tumor cells. The present invention furthermore relates to pharmaceutical compositions comprising the compounds and the use of the compounds for a treatment of diseases, in particular cancer and neurodegenerative diseases.

主权项

1. A compound having the formula wherein R1 is Boc, Z, Ac or H, Z is benzyloxycarbonyl, L is Leu, X is Leu or Asp(OR4), R2 is CH2—CH(CH3)2, R3 is CH2—OH, CH═O, CH(OH)—C≡C-phenyl, CH(OH)—C(O)—NH—R5 or C(O)—C(O)—NH—R5, R4 is t-butyl, benzyl or H, and R5 is benzyl, 3-picolyl or phenyl, with the exception of a compound wherein X is Leu and R3 is CH═O, and with the exception of a compound wherein X is Leu, R1 is Ac and R3 is CH2—OH, and pharmaceutically acceptable salts thereof.