کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1377389 | 981977 | 2007 | 5 صفحه PDF | دانلود رایگان |

Structure–activity relationship studies on a series of Boc-indole derivatives as LXR agonists are described. Compound 1 was identified as an LXR agonist through structure-based virtual screening followed by high-throughput gene profiling. Replacement of the indan linker portion in 1 with an open-chain linker resulted in compounds with similar or improved in vitro potency and cellular functional activity. The Boc group at the N-1 position of the indole moiety can be replaced with a benzoyl group. The SAR studies led to the identification of compound 8, a potent LXRβ agonist with an EC50 of 12 nM in the cofactor recruitment assay.
SAR studies on HTS hit compound 1 led to the identification of simpler 2-aryl-1-acyl compounds such as 8 which are potent LXRβ agonists.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 16, 15 August 2007, Pages 4442–4446