Design, synthesis, and biological evaluation of 2-aminobenzanilide derivatives as potent and selective HDAC inhibitors. (Articolo in rivista)

Type

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

Label

• Design, synthesis, and biological evaluation of 2-aminobenzanilide derivatives as potent and selective HDAC inhibitors. (Articolo in rivista) (literal)

Anno

• 2012-01-01T00:00:00+01:00 (literal)

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

• 10.1002/cmdc.201200193 (literal)

Alternative label

• Stolfa DA, Stefanachi A, Gajer JM, Nebbioso A, Altucci L, Cellamare S, Jung M, Carotti A. (2012)
  Design, synthesis, and biological evaluation of 2-aminobenzanilide derivatives as potent and selective HDAC inhibitors.
  in ChemMedChem (Print)
  (literal)

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

• Stolfa DA, Stefanachi A, Gajer JM, Nebbioso A, Altucci L, Cellamare S, Jung M, Carotti A. (literal)

Pagina inizio

• 1256 (literal)

Pagina fine

• 1266 (literal)

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

• 7 (literal)

Rivista

• ChemMedChem (Rivista)

Note

• PubMe (literal)

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

• Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstr. 25, 79104 Freiburg (Germany) Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Università degli Studi di Bari \"A. Moro\", Via Orabona 4, 70125 Bari (Italy) Department of General Pathology, Seconda Università di Napoli, Vico L. De Crecchio 7, 80138 Napoli (Italy) CNR-IGB \"ABT\", Via P. Castellino 111, 80131 Napoli (Italy) (literal)

Titolo

• Design, synthesis, and biological evaluation of 2-aminobenzanilide derivatives as potent and selective HDAC inhibitors. (literal)

Abstract

• Epigenetic regulation is an essential process for the normal functioning of genes. Therefore, targeting epigenetic dysregulation in cancer may be a valid therapeutic approach for the treatment of this severe disease. Histone deacetylases (HDACs) are enzymes involved in the regulation of epigenetic post-translational modifications; because they are overexpressed in many types of cancer, HDACs are valuable targets for the development of new anticancer agents. A large series of 2-aminobenzanilides linked at the 4'-position to ?-amino acid amides, arenes, and heteroarenes through a methylene bridge were designed, synthesized, and tested as novel HDAC inhibitors. Several compounds showed IC(50) values in the two-digit nanomolar range in hrHDAC1 inhibition assays, lower than that of the reference compound MS-275. They also showed interesting selectivity profiles, as confirmed by western blot assays. (literal)

Prodotto di

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

Autore CNR

• Lucia Altucci (Unità di personale esterno)

Incoming links:

Prodotto

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

Autore CNR di

• Lucia Altucci (Unità di personale esterno)

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

• ChemMedChem (Rivista)