N-Hydroxy-(4-oxime)-cinnamide: A versatile scaffold for the synthesis of novel histone deacetilase (HDAC) inhibitors

被引：32

作者：

Giannini, Giuseppe ^{[1
]}

Marzi, Mauro ^{[1
]}

Pezzi, Riccardo ^{[1
]}

Brunetti, Tiziana ^{[1
]}

Battistuzzi, Gianfranco ^{[1
]}

Di Marzo, Maria ^{[1
]}

Cabri, Walter ^{[1
]}

Vesci, Loredana ^{[1
]}

Pisano, Claudio ^{[1
]}

机构：

[1] R&D Sigma Tau SpA, I-00040 Pomezia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 08期

关键词：

HDAC inhibitors; Cinnamide; Hydroxamic acids; Antitumor; DEACETYLASE INHIBITORS; AGENTS;

D O I：

10.1016/j.bmcl.2009.02.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

With the aim to discover novel HDAC inhibitors with high potency and good safety profiles, we have designed a small library based on a N-hydroxy-(4-oxime)-cinnamide scaffold. We describe the synthesis of these novel compounds and some preliminary in vitro cytotoxic activity on three tumor cell lines, NB4, H460 and HCT116, as well as their inhibitory activity against class I, II and IV HDAC. Several 4-oxime derivatives demonstrated a promising inhibitory activity on HDAC6 and HDAC8 coupled to a good selectivity profile. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2346 / 2349

页数：4

共 20 条

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