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

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 different...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-07, Vol.57 (14), p.6259-6265
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Proliferation - drug effects Dose-Response Relationship, Drug Doxorubicin - pharmacology Drug Screening Assays, Antitumor HCT116 Cells Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology HL-60 Cells Humans Molecular Structure Oxadiazoles - chemical synthesis Oxadiazoles - chemistry Oxadiazoles - pharmacology Structure-Activity Relationship Tumor Cells, Cultured
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm500303u