New aryldithiolethione derivatives as potent histone deacetylase inhibitors

被引：19
|
作者：
Tazzari, Valerio [1 ]
Cappelletti, Graziella [2 ]
Casagrande, Manolo [3 ]
Perrino, Elena [1 ]
Renzi, Luigi [3 ]
Del Soldato, Piero [1 ]
Sparatore, Anna [1 ,3 ]
机构：
[1] Sulfidris Srl, I-20131 Milan, Italy
[2] Univ Milan, Dept Biol, I-20133 Milan, Italy
[3] Univ Milan, Dept Pharmaceut Sci Pietro Pratesi, I-20133 Milan, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 12期
关键词：
Histone deacetylase inhibitor; Dithiolethione derivatives; Anticancer agents; HYDROGEN-SULFIDE; CANCER-THERAPY; RAT; INDUCTION; ACID; 3H-1,2-DITHIOLE-3-THIONE; CARDIOPROTECTION; MODULATION; PROTECTION; TOXICITY;
D O I：
10.1016/j.bmc.2010.05.011
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of dithiolethione derivatives was synthesized and the in vitro HDAC inhibitory activity was tested. The most active compounds, 1 and 2, exhibited an IC50 in nM range with a strong hyperacetylation of histone H4 in A549 cells. The HDAC inhibitory activity comparable to that of SAHA and the inhibition of A549 cell proliferation suggest that these compounds are worthy of further studies as potential anticancer agents. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4187 / 4194
页数：8
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