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Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125. Epub 2012 Feb 8.

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

Author information

1
Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France. olivier.x.mirguet@gsk.com

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.

PMID:
22386529
DOI:
10.1016/j.bmcl.2012.01.125
[Indexed for MEDLINE]

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