N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors

被引：48

作者：

Kiviranta, Paivi H.

Leppanen, Jukka

Rinne, Valtteri M.

Suuronen, Tiina

Kyrylenko, Olga

Kyrylenko, Sergly

Kuusisto, Erkki

Tervo, Anu J.

Jarvinen, Tomi

Salminen, Antero

Poso, Antti

Wallen, Erik A. A.

机构：

[1] Univ Kuopio, Dept Pharmaceut Chem, FIN-70211 Kuopio, Finland

[2] Univ Kuopio, Dept Neurol & Neurosci, FIN-70211 Kuopio, Finland

[3] Kuopio Univ Hosp, Dept Neurol, Kuopio 70211, Finland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 09期

基金：

芬兰科学院;

关键词：

SIRT2; HDAC; inhibitor;

D O I：

10.1016/j.bmcl.2007.02.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides was based on a previously reported new SIRT2 inhibitor from our group, and it was designed to study if the molecular size of the compound could be reduced. The most potent compounds, N-(3-(4-hydroxyphenyl)-propenoyl)-2-aminoisobutyric acid tryptamide and N-(3-(4-hydroxyphenyl)-propenoyl)-L-alanine tryptamide, were equipotent, 30% smaller in molecular weight, and slightly more selective (SIRT2/SIRT1) than the parent compound. (C) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2448 / 2451

页数：4

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