Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

Farid Bakir,Sunil Kher,Madhavi Pannala,Norma Wilson,Trang Nguyen,Ila Sircar,Kei Takedomi,Chiaki Fukushima,James Zapf,Kui Xu,Shao-Hui Zhang,Juping Liu,Lisa Morera,Lisa Schneider,Naoki Sakurai,Rick Jack,Jie-Fei Cheng

doi:10.1016/j.bmcl.2007.03.076

Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

Farid Bakir, Sunil Kher + Show 15 more

https://doi.org/10.1016/j.bmcl.2007.03.076

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Mar 27, 2007
Citations: 13

Affiliation: Tanabe Research Laboratories, Teikoku Seiyaku (Japan)

#Liver X Receptor #High-throughput Gene Profiling + Show 8 more

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Abstract

A structurally novel liver X receptor (LXR) agonist ( 1) was identified from internal compound collection utilizing the combination of structure-based virtual screening and high-throughput gene profiling. Compound 1 increased ABCA1 gene expression by eightfold and SREBP1c by threefold in differentiated THP-1 macrophage cell lines. Confirmation of its agonistic activity against LXR was obtained in the co-factor recruitment and reporter transactivation assays. Structure–activity relationship studies on compound 1 are described.

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