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

Basic Information

ID: ALA1149512

Journal: Bioorg Med Chem Lett

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

Authors: Rivkin A, Kim YR, Goulet MT, Bays N, Hill AD, Kariv I, Krauss S, Ginanni N, Strack PR, Kohl NE, Chung CC, Varnerin JP, Goudreau PN, Chang A, Tota MR, Munoz B.

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).

CiteXplore: 16784844

DOI: 10.1016/j.bmcl.2006.06.014

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