Fluorinated oxysterol analogues: Synthesis, molecular modelling and LXRβ activity

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• 作者：Cristian R. Rodriguez^a ; Lautaro D. Alvarez^a ; ¹ ; M.Virginia Dansey^a ; ¹ ; Luciano S. Paolo^b ; Adriana S. Veleiro^a ; Adali Pecci^b ; Gerardo Burton^a ; ^{burton@qo.fcen.uba.ar}
• 关键词：Oxysterols ; Cholestenoic acid ; Liver X receptor ; Molecular dynamics
• 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：268-276
• 全文大小：1876 K
• 卷排序：165

文摘

Difluoro-oxysterols were prepared by Reformatsky reaction with ultrasound irradiation. 25,25-Difluoro-27-norcholestenoic acid was an inverse agonist and antagonist of LXRβ. 25,25-Difluoro-27-nor-26-hydroxycholesterol was an agonist of LXRβ. The fluorine atoms of the difluoroalcohol help stabilize the LXR agonist conformation.