Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells (Articolo in rivista)

Type
Label
  • Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells (Articolo in rivista) (literal)
Anno
  • 2014-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1002/cmdc.201300536 (literal)
Alternative label
  • Lenoci, Alessia; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Rodriguez, Veronica; Carradori, Simone; Secci, Daniela; Castellano, Sabrina; Sbardella, Gianluca; Filetici, Patrizia; Novellino, Ettore; Altucci, Lucia; Rotili, Dante; Mai, Antonello (2014)
    Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells
    in ChemMedChem (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Lenoci, Alessia; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Rodriguez, Veronica; Carradori, Simone; Secci, Daniela; Castellano, Sabrina; Sbardella, Gianluca; Filetici, Patrizia; Novellino, Ettore; Altucci, Lucia; Rotili, Dante; Mai, Antonello (literal)
Pagina inizio
  • 542 (literal)
Pagina fine
  • 548 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 9 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 7 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 3 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Department of Drug Chemistry & Technologies, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome (Italy) Department of Pharmacy, University of Naples \"Federico II\", Via D. Montesano 49, 80131 Naples (Italy) Department of Biochemistry, Biophysics & General Pathology, Second University of Naples, Vico L. De Crecchio 7, 80138 Naples (Italy) Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano (SA) (Italy) Laboratory of Nucleic Acids, Institute of Molecular Biology & Pathology (CNR-IBPM), Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome (Italy) Institute of Genetics & Biophysics (CNR-IGB), Via P. Castellino 111, 80131 Naples (Italy) Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome (Italy) (literal)
Titolo
  • Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells (literal)
Abstract
  • Chemical manipulations performed on 2-methyl-3-carbethoxyquinoline (1), a histone acetyltransferase inhibitor previously identified by our research group and active at the sub-millimolar/millimolar level, led to compounds bearing higher alkyl groups at the C2-quinoline or additional side chains at the C6-quinoline positions. Such compounds displayed at least threefold improved inhibitory potency toward p300 protein lysine acetyltransferase activity; some of them decreased histone H3 and H4 acetylation levels in U937 cells and induced high degrees of apoptosis (three compounds >10-fold higher than compound 1) after treatment of U937 cells. (literal)
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