title: 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
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.
authors: Department of Drug Chemistry and Technologies, Sapienza University of Rome , P. le A. Moro 5, 00185 Rome Italy.
authors: Sergio
authors: S
authors: Valente
authors: Daniela
authors: D
authors: Trisciuoglio
authors: Teresa
authors: T
authors: De Luca
authors: Angela
authors: A
authors: Nebbioso
authors: Donatella
authors: D
authors: Labella
authors: Alessia
authors: A
authors: Lenoci
authors: Chiara
authors: C
authors: Bigogno
authors: Giulio
authors: G
authors: Dondio
authors: Marco
authors: M
authors: Miceli
authors: Gerald
authors: G
authors: Brosch
authors: Donatella
authors: D
authors: Del Bufalo
authors: Lucia
authors: L
authors: Altucci
authors: Antonello
authors: A
authors: Mai
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D018922:HL-60 Cells; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D010069:Oxadiazoles; C583463:1,3,4-oxadiazole; D004317:Doxorubicin