2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
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Kher S, Lake K, Sircar I, Pannala M, Bakir F, Zapf J, Xu K, Zhang SH, Liu J, Morera L, Sakurai N, Jack R, Cheng JF
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4442-6. Epub 2007 Jun 10.
- PubMed ID
- 17587573 [ View in PubMed]
- Abstract
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 LXRbeta agonist with an EC50 of 12 nM in the cofactor recruitment assay.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) TO-901317 Oxysterols receptor LXR-alpha EC 50 (nM) 40 7.5 22 Details