1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells
| Autor: | Marco Miceli, Antonello Mai, Gerald Brosch, Alessia Lenoci, Donatella Del Bufalo, Angela Nebbioso, Lucia Altucci, Giulio Dondio, Daniela Trisciuoglio, Sergio Valente, Teresa De Luca, Donatella Labella, Chiara Bigogno |
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| Přispěvatelé: | Valente, S, Trisciuoglio, D, De Luca, T, Nebbioso, Angela, Labella, D, Lenoci, A, Bigogno, C, Dondio, G, Miceli, M, Brosch, G, Del Bufalo, D, Altucci, Lucia, Mai, A. |
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Cellular differentiation
Antineoplastic Agents HL-60 Cells Structure-Activity Relationship hemic and lymphatic diseases Drug Discovery medicine Tumor Cells Cultured cancer Humans hDAC inhibitors Cell Proliferation Oxadiazoles U937 cell Dose-Response Relationship Drug Molecular Structure Chemistry Myeloid leukemia medicine.disease HCT116 Cells HDAC1 Histone Deacetylase Inhibitors Leukemia Cell culture Doxorubicin Cancer cell Cancer research Molecular Medicine Histone deacetylase Drug Screening Assays Antitumor epigenetic |
| Zdroj: | Journal of medicinal chemistry 57 (2014): 6259–6265. doi:10.1021/jm500303u info:cnr-pdr/source/autori: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/titolo:1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells/doi:10.1021%2Fjm500303u/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:6259/pagina_a:6265/intervallo_pagine:6259–6265/volume:57 |
| DOI: | 10.1021/jm500303u |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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