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). (C) 2012 Elsevier Ltd. All rights reserved.
Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
[EN] MULTICATALYTIC PROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE PROTEASE MULTICATALYTIQUE
申请人:CEPHALON, INC.
公开号:WO1996014857A1
公开(公告)日:1996-05-23
(EN) Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by general formula (I). Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.(FR) Cette invention se rapporte à des inhibiteurs de l'enzyme protéase multicatalytique, lesquels sont représentés de manière générale par la formule suivante (I). Les éléments constituants ainsi que les éléments constituants préférés sont présentés dans la description de cette invention. Les méthodes concernant la fabrication et l'emploi de ces composés sont également exposées dans la description de cette invention.