4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 8, Pages 2963-2967

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.125

Keywords

ApoA1 upregulators; 7-Isoxazoloquinolines; BET family; Bromodomains inhibitors

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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. (C) 2012 Elsevier Ltd. All rights reserved.

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