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Updated: Apr 27, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells
Sergio Valente1, Daniela Trisciuoglio, Teresa De Luca
1Department of Drug Chemistry and Technologies, Sapienza University of Rome , P. le A. Moro 5, 00185 Rome Italy.
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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