1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells
Journal of Medicinal Chemistry2014Vol. 57(14), pp. 6259–6265
Citations Over TimeTop 10% of 2014 papers
Sérgio Valente, 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
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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