Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride …

…, V Clerin, SJ Gardell, P Nambi, E Quinet…

文献索引：Wrobel, Jay; Steffan, Robert; Bowen, S. Marc; Magolda, Ronald; Matelan, Edward; Unwalla, Rayomand; Basso, Michael; Clerin, Valerie; Gardell, Stephen J.; Nambi, Ponnal; Quinet, Elaine; Reminick, Jason I.; Vlasuk, George P.; Wang, Shuguang; Feingold, Irene; Huselton, Christine; Bonn, Tomas; Farnegardh, Mathias; Hansson, Tomas; Nilsson, Annika Goos; Wilhelmsson, Anna; Zamaratski, Edouard; Evans, Mark J. Journal of Medicinal Chemistry, 2008 , vol. 51, # 22 p. 7161 - 7168

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被引用次数: 46

摘要

A series of substituted 2-benzyl-3-aryl-7-trifluoromethylindazoles were prepared as LXR modulators. These compounds were partial agonists in transactivation assays when compared to 1 (T0901317) and were slightly weaker with respect to potency and efficacy on LXRα than on LXRβ. Lead compounds in this series 12 (WAY-252623) and 13 (WAY- 214950) showed less lipid accumulation in HepG2 cells than potent full agonists 1 and 3 ( ...