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Title

Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors

Authors
Musso, Loana
Cincinelli, Raffaella
Zuco, Valentina
Zunino, Franco
Giannini, Giuseppe
Vesci, Loredana
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Published in Bioorganic & Medicinal Chemistry Letters. 2015, vol. 25, no. 20, p. 4457-4460
Abstract A series of alternative Zn-binding groups were explored in the design of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. Most of the synthesized compounds were less effective than the parent hydroxamic acid. However, the profile of activity shown by the analog bearing a hydroxyurea head group, makes this derivative promising for further investigation.
Keywords Cell LineTumorCell Proliferation/drug effectsDose-Response RelationshipDrugHistone Deacetylase 2/antagonists & inhibitors/metabolismHistone Deacetylase Inhibitors/chemical synthesis/chemistry/pharmacologyHumansHydroxamic Acids/chemistry/pharmacologyModelsMolecularMolecular StructureOrganometallic Compounds/chemical synthesis/chemistry/pharmacologyStructure-Activity RelationshipZinc/chemistry/pharmacology
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PMID: 26376355
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MUSSO, Loana et al. Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors. In: Bioorganic & Medicinal Chemistry Letters, 2015, vol. 25, n° 20, p. 4457-4460. https://archive-ouverte.unige.ch/unige:94981

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Deposited on : 2017-06-20

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