Syntheses of amamistatin fragments and determination of their HDAC and antitumor activity

被引:35
作者
Fennell, Kelley A. [1 ]
Miller, Marvin J.
机构
[1] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA
[2] Univ Notre Dame, Walter Canc Ctr, Notre Dame, IN 46556 USA
[3] Hans Knoll Inst, Leibniz Inst Nat Prod Res & Infect Biol, D-07745 Jena, Germany
关键词
D O I
10.1021/ol070382e
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Amamistatins A and B are natural products found to have anti-proliferative effects against MCF-7, A549, and MKN45 human tumor cell lines (IC(50) 0.24-0.56 mu M). It was proposed that their activity was due to histone deacetylase (HDAC) inhibition mediated by the N-formyl-N-hydroxy lysine moiety. Amamistatin B fragment analogs were synthesized and screened for biological activity. These compounds were modest HDAC inhibitors and showed antitumor activity against MCF-7 and PC-3 human tumor cells.
引用
收藏
页码:1683 / 1685
页数:3
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