title: Discovery and Synthesis of a Novel Series of Liver X Receptor Antagonists.
abstract: Fourteen novel compounds were prepared and their antagonistic activities against liver X receptors (LXR) α/β were tested in vitro. Compound 26 had an IC50 value of 6.4 µM against LXRα and an IC50 value of 5.6 µM against LXRβ. Docking studies and the results of structure-activity relationships support the further development of this chemical series as LXRα/β antagonists.
authors.affiliation: Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry.
authors.forename: Siyun
authors.initials: S
authors.lastname: Nian
authors.forename: Xia
authors.initials: X
authors.lastname: Gan
authors.forename: Xiangduan
authors.initials: X
authors.lastname: Tan
authors.forename: Zhenpeng
authors.initials: Z
authors.lastname: Yu
authors.forename: Panfeng
authors.initials: P
authors.lastname: Wang
authors.forename: Xing
authors.initials: X
authors.lastname: Chen
authors.forename: Guoping
authors.initials: G
authors.lastname: Wang
mesh_terms: D055808:Drug Discovery; D011345:Fenofibrate / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D000071518:Liver X Receptors; D062105:Molecular Docking Simulation; D057093:Orphan Nuclear Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000960:Hypolipidemic Agents; D008024:Ligands; D000071518:Liver X Receptors; C000605213:NR1H3 protein, human; D057093:Orphan Nuclear Receptors; D011345:Fenofibrate