Synthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptors

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• 作者：Ove Alexander H&oslash ; gmoen Å ; strand^a ; Elvar Ö ; rn Viktorsson^a ; Aleksander Lim Kristensen^a ; Dag Ekeberg^b ; Hanne R&oslash ; berg-Larsen^c ; Steven Ray Wilson^c ; Mari Gabrielsen^d ; Ingebrigt Sylte^d ; Arild Christian Rustan^e ; G. Hege Thoresen^e ; ^f ; På ; l Rongved^a ; Eili Tranheim Kase^e ; ^{e.t.kase@farmasi.uio.no}
• 关键词：Steroid synthesis ; Nuclear receptor modulation ; Molecular modelling ; Biological evaluation
• 刊名：The Journal of Steroid Biochemistry and Molecular Biology
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：165
• 期：part_PB
• 页码：323-330
• 全文大小：1253 K
• 卷排序：165

文摘

Synthesis of new oxysterols as putative LXR modulators. In silico docking studies of the new LXR modulators. Two of the compounds showed promising results on lipogenesis, FASN, SCD1 and ABCA1 in vitro. In vivo evaluation of the seemingly best compound gave no deviation from control on weight gain or TAG.