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

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125.
Olivier Mirguet  1 ,  Yann Lamotte ,  Frédéric Donche ,  Jérôme Toum ,  Françoise Gellibert ,  Anne Bouillot ,  Romain Gosmini ,  Van-Loc Nguyen ,  Delphine Delannée ,  Jonathan Seal ,  Florence Blandel ,  Anne-Bénédicte Boullay ,  Eric Boursier ,  Sandrine Martin ,  Jean-Marie Brusq ,  Gael Krysa ,  Alizon Riou ,  Rémi Tellier ,  Agnès Costaz ,  Pascal Huet ,  Yann Dudit ,  Lionel Trottet ,  Jorge Kirilovsky ,  Edwige Nicodeme
Affiliations
  • 1. Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France. [email protected]
PMID: 22386529 DOI: 10.1016/j.bmcl.2012.01.125
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.

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