Articolo in rivista, 2014, ENG, 10.1021/jm500303u

1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

Valente, Sergio; Trisciuoglio, Daniela; De Luca, Teresa; Nebbioso, Angela; Labella, Donatella; Lenoci, Alessia; Bigogno, Chiara; Dondio, Giulio; Miceli, Marco; Brosch, Gerald; Del Bufalo, Donatella; Altucci, Lucia; Mai, Antonello

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome Italy Regina Elena National Cancer Institute, Via Elio Chianesi, 53, 00144 Rome, Italy Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, Vico L. De Crecchio 7, 80138 Naples, Italy Aphad Srl, Via della Resistanza 65, 20090 Buccinasco, Milan, Italy Division of Molecular Biology, Biocenter, Innsbruck Medical University, Innrain 80/III, 6020 Innsbruck, Austria CNR-IGB, Institute of Genetics and Biophysics, via P. Castellino, 80100 Naples, Italy Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza University of Rome, P. le A. Moro 5 00185, Rome, Italy

We describe 1,3,4-oxadiazole-containing hydroxamates (2) and 2-aminoanilides (3) as histone deacetylase inhibitors. Among them, 2t, 2x, and 3i were the most potent and selective against HDAC1. In U937 leukemia cells, 2t was more potent than SAHA in inducing apoptosis, and 3i displayed cell differentiation with a potency similar to MS-275. In several acute myeloid leukemia (AML) cell lines, as well as in U937 cells in combination with doxorubicin, 3i showed higher antiproliferative effects than SAHA.

Journal of medicinal chemistry 57 (14), pp. 6259–6265

Keywords

CNR authors

Altucci Lucia

CNR institutes

IGB – Istituto di genetica e biofisica "Adriano Buzzati Traverso"

ID: 287245

Year: 2014

Type: Articolo in rivista

Creation: 2014-11-17 12:00:08.000

Last update: 2015-11-24 18:21:45.000

CNR authors

External links

OAI-PMH: Dublin Core

OAI-PMH: Mods

OAI-PMH: RDF

DOI: 10.1021/jm500303u

External IDs

CNR OAI-PMH: oai:it.cnr:prodotti:287245

DOI: 10.1021/jm500303u

ISI Web of Science (WOS): 000339540800033