Synthesis, chemical characterization and biological activity of new histone acetylation/deacetylation specific inhibitors: A novel and potential approach to cancer therapy (Articolo in rivista)

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Label
  • Synthesis, chemical characterization and biological activity of new histone acetylation/deacetylation specific inhibitors: A novel and potential approach to cancer therapy (Articolo in rivista) (literal)
Anno
  • 2013-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.jinorgbio.2013.04.008 (literal)
Alternative label
  • Pellerito, Ornella; Prinzivalli, Cristina; Foresti, Elisabetta; Sabatino, Piera; Abbate, Michele; Casella, Girolamo; Fiore, Tiziana; Scopelliti, Michelangelo; Pellerito, Claudia; Giuliano, Michela; Grasso, Giulia; Pellerito, Lorenzo (2013)
    Synthesis, chemical characterization and biological activity of new histone acetylation/deacetylation specific inhibitors: A novel and potential approach to cancer therapy
    in Journal of inorganic biochemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Pellerito, Ornella; Prinzivalli, Cristina; Foresti, Elisabetta; Sabatino, Piera; Abbate, Michele; Casella, Girolamo; Fiore, Tiziana; Scopelliti, Michelangelo; Pellerito, Claudia; Giuliano, Michela; Grasso, Giulia; Pellerito, Lorenzo (literal)
Pagina inizio
  • 16 (literal)
Pagina fine
  • 25 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 125 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 10 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Policlin Univ; University of Palermo - Italy; University of Bologna; University of Palermo - Italy; University of Palermo - Italy; Consorzio Interuniv Ric Chim Met Sistemi Biol; Policlin Univ; Consiglio Nazionale delle Ricerche (CNR) (literal)
Titolo
  • Synthesis, chemical characterization and biological activity of new histone acetylation/deacetylation specific inhibitors: A novel and potential approach to cancer therapy (literal)
Abstract
  • Three new triorganotin(IV) complexes of valproic acid (vp1, Me3Sn-valproate; vp2, Bu3Sn-valproate; vp3, Ph3Sn-valproate) have been synthesized and investigated by spectroscopic and biological methods. An anionic, monodentate valproate ligand was observed, ester-like coordinating the tin atom on a tetra-coordinated, monomeric environment. The structures, though, can distort towards a penta-coordination, as a consequence of a long range O center dot center dot center dot Sn interaction. Crystallographic and NMR findings confirm this situation both in solid state and solution. Biological finding evidenced a clear cytotoxic action of the complexes in hepatocellular carcinoma cell cultures: one of the complexes induced an 80% cell viability reduction after 24 h treatment in HepG2 cells. This effect was accompanied by the appearance of biochemical signs of apoptosis. In Chang liver cells, the same compound induced only modest effects, suggesting a potential use as anti-cancer drug. Preliminary evaluations on hyperacetylation state of histone H3 in tributyltin-valproate treated HepG2 cells showed an increase in Ac-H3 (histone H3 acetylated at lys-9 and lys-14), suggesting that the compound maintains the deacetylation inhibition activity of its ligand valproate. (c) 2013 Elsevier Inc. All rights reserved. (literal)
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