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Discovery and Synthesis of Hydronaphthoquinones as Novel Proteasome Inhibitors

Screening efforts led to the identification of PI-8182 (1), an inhibitor of the chymotrypsin-like (CT-L) activity of the proteasome. Compound 1 contains a hydronaphthoquinone pharmacophore with a thioglycolic acid side chain at position 2 and thiophene sulfonamide at position 4. An efficient synthet...

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Detalhes bibliográficos
Main Authors: Ge, Yiyu, Kazi, Aslamuzzaman, Marsilio, Frank, Luo, Yunting, Jain, Sanjula, Brooks, Wesley, Daniel, Kenyon G., Guida, Wayne C., Sebti, Saïd M., Lawrence, Harshani R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3530929/
https://ncbi.nlm.nih.gov/pubmed/22220566
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm201118h
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