Fennell Kelley A, Miller Marvin J
Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, USA.
Org Lett. 2007 Apr 26;9(9):1683-5. doi: 10.1021/ol070382e. Epub 2007 Mar 31.
[reaction: see text] Amamistatins A and B are natural products found to have anti-proliferative effects against MCF-7, A549, and MKN45 human tumor cell lines (IC50 0.24-0.56 microM). 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.
[反应：见正文] 氨甲他汀A和B是天然产物，已发现它们对MCF-7、A549和MKN45人肿瘤细胞系具有抗增殖作用（IC50为0.24 - 0.56微摩尔）。有人提出它们的活性归因于由N-甲酰基-N-羟基赖氨酸部分介导的组蛋白脱乙酰酶（HDAC）抑制作用。合成了氨甲他汀B片段类似物并对其进行生物活性筛选。这些化合物是适度的HDAC抑制剂，并对MCF-7和PC-3人肿瘤细胞显示出抗肿瘤活性。
