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

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

Bioorganic & medicinal chemistry letters (2006-06-21)
Alexey Rivkin, Yoona R Kim, Mark T Goulet, Nathan Bays, Armetta D Hill, Ilona Kariv, Stefan Krauss, Nicole Ginanni, Peter R Strack, Nancy E Kohl, Christine C Chung, Jeffrey P Varnerin, Paul N Goudreau, Amy Chang, Michael R Tota, Benito Munoz
PMID16784844
ABSTRACT

A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC(50) = 1.4 microM, SAR studies led to compounds with more than 70-fold increase in potency (IC(50) < 20 nM).