Development of Novel Amides as Noncovalent Inhibitors of Immunoproteasomes.
amides
docking studies
immunoproteasomes
medicinal chemistry
noncovalent inhibitors
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
17 04 2019
17 04 2019
Historique:
received:
14
01
2019
revised:
04
03
2019
pubmed:
5
3
2019
medline:
9
1
2020
entrez:
5
3
2019
Statut:
ppublish
Résumé
The development of immunoproteasome-selective inhibitors is a promising strategy for treating hematologic malignancies, autoimmune and inflammatory diseases. In this context, we report the design, synthesis, and biological evaluation of a new series of amide derivatives as immunoproteasome inhibitors. Notably, the designed compounds act as noncovalent inhibitors, which might be a promising therapeutic option because of the lack of drawbacks and side effects associated with irreversible inhibition. Among the synthesized compounds, we identified a panel of active inhibitors with K
Identifiants
pubmed: 30829448
doi: 10.1002/cmdc.201900028
doi:
Substances chimiques
Amides
0
Proteasome Inhibitors
0
Protein Subunits
0
Proteasome Endopeptidase Complex
EC 3.4.25.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
842-852Informations de copyright
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.