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Naphthoquinone amino acid derivatives, synthesis and biological activity as proteasome inhibitors
- Source :
- Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 865-877 (2017)
- Publication Year :
- 2017
- Publisher :
- Taylor & Francis Group, 2017.
-
Abstract
- The ubiquitin-proteasome system has been largely investigated for its key role in protein degradation mechanisms that regulate both apoptosis and cell division. Because of their antitumour activity, different classes of proteasome inhibitors have been identified to date. Some of these compounds are currently employed in the clinical treatment of several types of cancer among which multiple myeloma. Here, we describe the design, chemistry, biological activity and modelling studies of a large series of amino acid derivatives linked to a naphthoquinone pharmacophoric group through variable spacers. Some analogues showed interesting inhibitory potency for the β1 and β5 subunits of the proteasome with IC50 values in the sub-µm range.
Details
- Language :
- English
- ISSN :
- 14756366, 14756374, and 30836727
- Volume :
- 32
- Issue :
- 1
- Database :
- Directory of Open Access Journals
- Journal :
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.3083672705d5484a8b6e0097fa75b946
- Document Type :
- article
- Full Text :
- https://doi.org/10.1080/14756366.2017.1334649