期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 32, 期 1, 页码 865-877出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1334649
关键词
Proteasome; naphthoquinone; amino acid derivatives; post-acidic inhibition
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 beta 1 and beta 5 subunits of the proteasome with IC50 values in the sub-mu m range.
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