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Title

Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates

Authors
Bouchet, Samuel
Martinet, Nadine
Lehotzky, Attila
Ovadi, Judit
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Published in Bioorganic & Medicinal Chemistry Letters. 2016, vol. 26, no. 1, p. 154-159
Abstract Conditions for the metathesis of alkenes in the convergent synthesis of HDAC inhibitors have been improved by continuous catalyst flow injection in the reaction media. Intermediate and target compounds obtained were tested for their ability to induce HDAC inhibition and tubulin acetylation, revealing the key role of the tert-butyloxycarbonyl (BOC) group for more HDAC6 selectivity. Molecular modelling added rationale for this BOC effect.
Keywords Alkenes/chemistryBenzamides/chemistryDose-Response RelationshipDrugFormic Acid Esters/chemistryHistone Deacetylase Inhibitors/chemistry/pharmacologyHistone Deacetylases/metabolismHumansHydroxamic Acids/chemistryModelsMolecularMolecular StructureStructure-Activity Relationship
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PMID: 26611919
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ZWICK, Vincent et al. Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates. In: Bioorganic & Medicinal Chemistry Letters, 2016, vol. 26, n° 1, p. 154-159. https://archive-ouverte.unige.ch/unige:94979

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Deposited on : 2017-06-20

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