Inhibitors of histone deacetylase 6 based on a novel 3-hydroxy-isoxazole zinc binding group.


Journal

Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203

Informations de publication

Date de publication:
Dec 2021
Historique:
entrez: 29 9 2021
pubmed: 30 9 2021
medline: 27 1 2022
Statut: ppublish

Résumé

Histone deacetylase 6 (HDAC6) is an established drug target for cancer treatment. Inhibitors of HDAC6 based on a hydroxamic acid zinc binding group (ZBG) are often associated with undesirable side effects. Herein, we describe the identification of HDAC6 inhibitors based on a completely new 3-hydroxy-isoxazole ZBG. A series of derivatives decorated with different aromatic or heteroaromatic linkers, and various cap groups were synthesised and biologically tested.

Identifiants

pubmed: 34583596
doi: 10.1080/14756366.2021.1981306
pmc: PMC8480759
doi:

Substances chimiques

Coordination Complexes 0
Histone Deacetylase Inhibitors 0
HDAC6 protein, human EC 3.5.1.98
Histone Deacetylase 6 EC 3.5.1.98
Zinc J41CSQ7QDS

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

2080-2086

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Auteurs

Pasquale Linciano (P)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Luca Pinzi (L)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Silvia Belluti (S)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Ugo Chianese (U)

Department of Precision Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy.

Rosaria Benedetti (R)

Department of Precision Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy.

Davide Moi (D)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Lucia Altucci (L)

Department of Precision Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy.
Biogem Institute of Molecular and Genetic Biology, Ariano Irpino, Italy.

Silvia Franchini (S)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Carol Imbriano (C)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Claudia Sorbi (C)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

Giulio Rastelli (G)

Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

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Classifications MeSH