3-aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors

被引：51

作者：

Rivkin, Alexey

Kim, Yoona R.

Goulet, Mark T.

Bays, Nathan

Hill, Armetta D.

Kariv, Ilona

Krauss, Stefan

Ginanni, Nicole

Strack, Peter R.

Kohl, Nancy E.

Chung, Christine C.

Varnerin, Jeffrey P.

Goudreau, Paul N.

Chang, Amy

Tota, Michael R.

Munoz, Benito

机构：

[1] Merck Res Labs, Dept Chem, Boston, MA 02115 USA

[2] Merck Res Labs, Dept Automated Lead Optimizat, Boston, MA 02115 USA

[3] Merck Res Labs, Dept Canc Biol & Therapeut, Boston, MA 02115 USA

[4] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 17期

关键词：

fatty acid synthase; cancer; apoptosis;

D O I：

10.1016/j.bmcl.2006.06.014

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 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC50 = 1.4 mu M, SAR studies led to compounds with more than 70-fold increase in potency (IC50 < 20 nM). (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4620 / 4623

页数：4

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