Cinnamoyl Compounds as Simple Molecules that Inhibit p300 Histone Acetyltransferase
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- 作者：Roberta Costi ; Roberto Di Santo ; Marino Artico ; Gaetano Miele ; Paola Valentini ; Ettore Novellino ; Anna Cereseto
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：April 19, 2007
- 年：2007
- 卷：50
- 期：8
- 页码：1973 - 1977
- 全文大小：163K
- 年卷期：v.50,no.8(April 19, 2007)
- ISSN：1520-4804
文摘
Cinnamoly compounds 1a-c and 2a-d were designed, synthesized, and in vitro tested as p300 inhibitors.At different degrees, all tested compounds were proven to inactivate p300, particularly, derivative 2c wasthe most active inhibitor, also showing high specificity for p300 as compared to other histone acetyltransferases. Most notably, 2c showed anti-acetylase activity in mammalian cells. These compounds represent anew class of synthetic inhibitors of p300, characterized by simple chemical structures.