1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

被引：129

作者：

Valente, Sergio ^{[1
]}

Trisciuoglio, Daniela ^{[2
]}

De Luca, Teresa ^{[2
]}

Nebbioso, Angela ^{[3
]}

Labella, Donatella ^{[1
]}

Lenoci, Alessia ^{[1
]}

Bigogno, Chiara ^{[4
]}

Dondio, Giulio ^{[4
]}

Miceli, Marco ^{[3
]}

Brosch, Gerald ^{[5
]}

Del Bufalo, Donatella ^{[2
]}

Altucci, Lucia ^{[3
,6
]}

Mai, Antonello ^{[1
,7
]}

机构：

[1] Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy

[2] Regina Elena Inst Canc Res, I-00144 Rome, Italy

[3] Univ Naples 2, Dept Biochem Biophys & Gen Pathol, I-80138 Naples, Italy

[4] Aphad Srl, I-20090 Milan, Italy

[5] Med Univ Innsbruck, Bioctr, Div Mol Biol, A-6020 Innsbruck, Austria

[6] CNR, IGB, I-80100 Naples, Italy

[7] Univ Roma La Sapienza, Fdn Cenci Bolognetti, Ist Pasteur, I-00185 Rome, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 14期

关键词：

LEUKEMIA-CELLS; HDAC INHIBITORS; APOPTOSIS; ACETYLATION; INDUCTION; THERAPY; TRAIL;

D O I：

10.1021/jm500303u

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：6259 / 6265

页数：7

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