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Title

Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity

Authors
Cincinelli, Raffaella
Musso, Loana
Zuco, Valentina
De Cesare, Michelandrea
Zunino, Franco
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Published in European Journal of Medicinal Chemistry. 2016, vol. 112, p. 99-105
Abstract Modification of the cap group of biphenylacrylohydroxamic acid-based HDAC inhibitors led to the identification of a new derivative (3) characterized by an indolyl-substituted 4-phenylcinnamic skeleton. Molecular docking was used to predict the optimal conformation in the class I HDACs active site. Compound 3 showed HDAC inhibitory activity and antiproliferative activity against a panel of tumor cell lines, in the low μM range. The compound was further tested in vitro for acetylation of histone H4 and other non-histone proteins, and in vivo in a colon carcinoma model, showing significant proapoptotic and antitumor activities.
Keywords Antineoplastic Agents/chemistry/pharmacologyApoptosis/drug effectsBiphenyl Compounds/chemistry/pharmacologyColonic Neoplasms/drug therapy/metabolismDrug Screening AssaysAntitumorHCT116 CellsHistone Deacetylase Inhibitors/chemistry/pharmacologyHistone Deacetylases/metabolismHumansHydroxamic Acids/chemistry/pharmacologyMolecular Docking SimulationNeoplasms/drug therapy/metabolismStructure-Activity Relationship
Identifiers
PMID: 26890116
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CINCINELLI, Raffaella et al. Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. In: European Journal of Medicinal Chemistry, 2016, vol. 112, p. 99-105. https://archive-ouverte.unige.ch/unige:94976

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Deposited on : 2017-06-20

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