4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists

Bioorganic & Medicinal Chemistry Letters
Ronald C BernotasJay Wrobel

Abstract

A series of 4-(3-aryloxyaryl)quinolines with sulfone substituents on the terminal aryl ring (7) was prepared as LXR agonists. High affinity LXR ligands with excellent agonist potency and efficacy in functional assays of LXR activity were identified. In general, these sulfone agonists were equal to or superior to previously described alcohol and amide analogs in terms of affinity, functional potency, and microsomal stability. Many of the sulfones had LXRbeta binding IC(50) values <10nM while the most potent compounds in an ABCA1 mRNA induction assay in J774 mouse cells had EC(50) values <10nM and were as efficacious as T0901317.

References

Aug 5, 2004·Journal of Lipid Research·Elaine M QuinetPonnal Nambi
Apr 14, 2009·Chemical Reviews·José Marco-ContellesElena Soriano
Oct 27, 2009·Bioorganic & Medicinal Chemistry·Ronald C BernotasJay Wrobel

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Citations

Mar 26, 2011·Journal of Chemical Information and Modeling·Wenxia ZhaoJun Xu
Dec 17, 2009·Bioorganic & Medicinal Chemistry Letters·Robert R SinghausJay Wrobel
Dec 17, 2009·Bioorganic & Medicinal Chemistry Letters·Jeremy M TravinsJay Wrobel
Jan 19, 2010·Angewandte Chemie·Masayuki WasaJin-Quan Yu
Mar 19, 2016·Journal of Medicinal Chemistry·Ya-Jun ZhengSuresh B Singh
Jul 6, 2013·Expert Opinion on Therapeutic Patents·Jon LorenValentina Molteni
May 7, 2015·Bioconjugate Chemistry·Reyna K V LimStephanie A Kazane
Jan 4, 2017·Bioorganic & Medicinal Chemistry·Natália Aparecida LibertoSergio Antonio Fernandes
Mar 23, 2010·Expert Opinion on Therapeutic Patents·Xiaolin LiValentina Molteni
Jan 10, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rajesh KomatiGuangdi Wang
Aug 9, 2018·Frontiers in Pharmacology·Ming ChuYuedan Wang
May 17, 2014·Journal of Medicinal Chemistry·Colin M TiceSuresh B Singh
Apr 12, 2012·Journal of Chemical Information and Modeling·Susanne von GrafensteinDaniela Schuster
Jun 14, 2019·Journal of Chemical Information and Modeling·Peng DingJun Xu
Jul 14, 2018·Journal of Medicinal Chemistry·Bahaa El-Dien M El-GendyThomas P Burris
Apr 13, 2010·Bioorganic & Medicinal Chemistry Letters·John W UllrichJay Wrobel

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