Abstract
Proteasome, a large multicatalytic proteinase complex that plays an important role in processing of proteins, has been shown to possess multiple catalytic activities. Among its various activities, the 'chymotrypsin-like' activity of proteasome has emerged as the focus of drug discovery efforts in cancer therapy. Herein we report chiral boronate derived novel, potent, selective and cell-permeable peptidomimetic inhibitors 6 and 7 that displayed activity against various rodent and human tumor cell lines (in vitro).
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
-
Animals
-
Boronic Acids / chemistry*
-
Boronic Acids / pharmacology
-
Boronic Acids / therapeutic use
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
Drug Screening Assays, Antitumor
-
Humans
-
Liver / enzymology
-
Mice
-
Neoplasms / drug therapy
-
Nitro Compounds / chemistry*
-
Nitro Compounds / pharmacology
-
Nitro Compounds / therapeutic use
-
Protease Inhibitors / chemistry*
-
Protease Inhibitors / pharmacology
-
Protease Inhibitors / therapeutic use
-
Proteasome Endopeptidase Complex / metabolism
-
Proteasome Inhibitors*
Substances
-
Boronic Acids
-
Nitro Compounds
-
Protease Inhibitors
-
Proteasome Inhibitors
-
Proteasome Endopeptidase Complex