Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies (Articolo in rivista)

Type

• Prodotto della ricerca (Classe)
• Articolo in rivista (Classe)

Label

• Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies (Articolo in rivista) (literal)

Anno

• 2014-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1016/j.ejmech.2014.04.042 (literal)

Alternative label

• Carradori, Simone; Rotili, Dante; De Monte, Celeste; Lenoci, Alessia; D'Ascenzio, Melissa; Rodriguez, Veronica; Filetici, Patrizia; Miceli, Marco; Nebbioso, Angela; Altucci, Lucia; Secci, Daniela; Mai, Antonello (2014)
  Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies
  in European journal of medicinal chemistry
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Carradori, Simone; Rotili, Dante; De Monte, Celeste; Lenoci, Alessia; D'Ascenzio, Melissa; Rodriguez, Veronica; Filetici, Patrizia; Miceli, Marco; Nebbioso, Angela; Altucci, Lucia; Secci, Daniela; Mai, Antonello (literal)

Pagina inizio

• 569 (literal)

Pagina fine

• 578 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 80 (literal)

Rivista

• European journal of medicinal chemistry (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

• Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy Institute of Molecular Biology and Pathology (IBPM), CNR National Research Council of Italy, c/o Sapienza Università di Roma, 00185 Rome, Italy Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, vico L. De Crecchio 7, 80138 Naples, Italy CNR-IGB, Institute of Genetics and Biophysics, via P. Castellino, 80100 Naples, Italy Pasteur Institute, Cenci Bolognetti Foundation, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy (literal)

Titolo

• Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies (literal)

Abstract

• Recently we described some (thiazol-2-yl)hydrazones as antiprotozoal, antifungal and anti-MAO agents as well as Gcn5 HAT inhibitors. Among these last compounds, CPTH2 and CPTH6 showed HAT inhibition in cells and broad anticancer properties. With the aim to identify HAT inhibitors more potent than the two prototypes, we synthesized several new (thiazol-2-yl)hydrazones including some related thiazolidines and pyrimidin-4(3H)-ones, and we tested the whole library existing in our lab against human p300 and PCAF HAT enzymes. Some compounds (1x, 1c', 1d', 1i' and 2m) were more efficient than CPTH2 and CPTH6 in inhibiting the p300 HAT enzyme. When tested in human leukemia U937 and colon carcinoma HCT116 cells (100 mu M, 30 h), 1x, 1i' and 2m gave higher (U937 cells) or similar (HCT116 cells) apoptosis than CPTH6, and were more potent than CPTH6 in inducing cytodifferentiation (U937 cells). (C) 2014 Elsevier Masson SAS. All rights reserved. (literal)

Prodotto di

• Identificazione di regolatori del differenziamento, della motilità e dell'apoptosi delle cellule staminali (SV.P15.008.001) (Modulo)
• Istituto di genetica e biofisica \"Adriano Buzzati Traverso\" (IGB) (Istituto)

Autore CNR

• Lucia Altucci (Unità di personale esterno)
• PATRIZIA FILETICI (Unità di personale interno)

Insieme di parole chiave

• Keywords of "Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies" (Insieme di parole chiave)

Incoming links:

Autore CNR di

• PATRIZIA FILETICI (Unità di personale interno)
• Lucia Altucci (Unità di personale esterno)

Prodotto

• Istituto di genetica e biofisica \"Adriano Buzzati Traverso\" (IGB) (Istituto)
• Identificazione di regolatori del differenziamento, della motilità e dell'apoptosi delle cellule staminali (SV.P15.008.001) (Modulo)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• European journal of medicinal chemistry (Rivista)

Insieme di parole chiave di

• Keywords of "Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies" (Insieme di parole chiave)