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Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity |
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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/pharmacology — Apoptosis/drug effects — Biphenyl Compounds/chemistry/pharmacology — Colonic Neoplasms/drug therapy/metabolism — Drug Screening Assays — Antitumor — HCT116 Cells — Histone Deacetylase Inhibitors/chemistry/pharmacology — Histone Deacetylases/metabolism — Humans — Hydroxamic Acids/chemistry/pharmacology — Molecular Docking Simulation — Neoplasms/drug therapy/metabolism — Structure-Activity Relationship | |
Identifiers | PMID: 26890116 | |
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Citation (ISO format) | 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. doi: 10.1016/j.ejmech.2016.02.001 https://archive-ouverte.unige.ch/unige:94976 |