1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
Basic Information
ID: ALA3351281
Journal: J Med Chem
Title: 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
Authors: Valente S, Trisciuoglio D, De Luca T, Nebbioso A, Labella D, Lenoci A, Bigogno C, Dondio G, Miceli M, Brosch G, Del Bufalo D, Altucci L, Mai A.
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.
CiteXplore: 24972008
DOI: 10.1021/jm500303u
Patent ID: ┄