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. 2014 Jul 24;57(14):6259-65.
doi: 10.1021/jm500303u. Epub 2014 Jul 8.

1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells

Sergio Valente  1 , Daniela Trisciuoglio, Teresa De Luca, Angela Nebbioso, Donatella Labella, Alessia Lenoci, Chiara Bigogno, Giulio Dondio, Marco Miceli, Gerald Brosch, Donatella Del Bufalo, Lucia Altucci, Antonello Mai
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1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells

Sergio Valente et al. J Med Chem. .

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.

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