Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors

被引:18
作者
Angibaud, P
Arts, J
Van Emelen, K
Poncelet, V
Pilatte, I
Roux, B
Van Brandt, S
Verdonck, M
De Winter, H
Ten Holte, P
Marien, A
Floren, W
Janssens, B
Van Dun, J
Aerts, A
Van Gornpel, J
Gaurrand, S
Queguiner, L
Argoullon, JM
Van Hijfte, L
Freyne, E
Janicot, M
机构
[1] Johnson & Johnson Pharmaceut Res & Dev, Dept Med Chem, F-27106 Reuil, France
[2] Oncol Discovery Res, B-2340 Beerse, Belgium
[3] Dept Med Chem, B-2340 Beerse, Belgium
[4] Preclin Pharmacokinet, B-2340 Beerse, Belgium
关键词
histone deacetylase; hydroxamic acid; anticancer agents;
D O I
10.1016/j.ejmech.2005.01.008
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency. (c) 2005 Elsevier SAS. All rights reserved.
引用
收藏
页码:597 / 606
页数:10
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