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ID: ALA2016443

Journal: Bioorg Med Chem Lett

Title: From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

Authors: Mirguet O, Lamotte Y, Donche F, Toum J, Gellibert F, Bouillot A, Gosmini R, Nguyen VL, Delannée D, Seal J, Blandel F, Boullay AB, Boursier E, Martin S, Brusq JM, Krysa G, Riou A, Tellier R, Costaz A, Huet P, Dudit Y, Trottet L, Kirilovsky J, Nicodeme E.

Abstract: The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2.

CiteXplore: 22386529

DOI: 10.1016/j.bmcl.2012.01.125