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1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells
- Source :
- 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
- Publication Year :
- 2014
- Publisher :
- American Chemical Society, [Easton, Pa.] , Stati Uniti d'America, 2014.
-
Abstract
- 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.
- Subjects :
- 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
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- 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
- Accession number :
- edsair.doi.dedup.....1ef6fa0a6448bf020104ae8557502636