Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones

被引:55
作者
Jose, B [1 ]
Oniki, Y [1 ]
Kato, T [1 ]
Nishino, N [1 ]
Sumida, Y [1 ]
Yoshida, M [1 ]
机构
[1] Kyushu Inst Technol, Grad Sch Life Sci & Syst Engn, Kitakyushu, Fukuoka 8080196, Japan
关键词
histone deacetylase; inhibitor; cyclic tetrapeptide; trifluoromethyl ketone; pentafluoroethyl ketone;
D O I
10.1016/j.bmcl.2004.08.016
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cyclic tetrapeptides containing trifluoromethyl and pentafluoroethyl ketone as zinc binding functional group were synthesized as potent HDAC inhibitors. Evaluation by human HDAC inhibition assay and p21 promoter assay showed that these inhibitors are promising anticancer agents. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5343 / 5346
页数:4
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