Literature DB >> 19167885

Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.

David G Washburn1, Tram H Hoang, Nino Campobasso, Angela Smallwood, Derek J Parks, Christine L Webb, Kelly A Frank, Melanie Nord, Chaya Duraiswami, Christopher Evans, Michael Jaye, Scott K Thompson.   

Abstract

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRalpha will be disclosed.

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Year:  2009        PMID: 19167885     DOI: 10.1016/j.bmcl.2009.01.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  The retinoid X receptors and their ligands.

Authors:  Marcia I Dawson; Zebin Xia
Journal:  Biochim Biophys Acta       Date:  2011-10-01

2.  Tri-m-cresyl phosphate and PPAR/LXR interactions in seabream hepatocytes: revealed by computational modeling (docking) and transcriptional regulation of signaling pathways.

Authors:  Francesco Alessandro Palermo; Paolo Cocci; Matteo Mozzicafreddo; Augustine Arukwe; Mauro Angeletti; Graziano Aretusi; Gilberto Mosconi
Journal:  Toxicol Res (Camb)       Date:  2015-12-18       Impact factor: 3.524

3.  Identification of novel liver X receptor activators by structure-based modeling.

Authors:  Susanne von Grafenstein; Judit Mihaly-Bison; Gerhard Wolber; Valery N Bochkov; Klaus R Liedl; Daniela Schuster
Journal:  J Chem Inf Model       Date:  2012-04-20       Impact factor: 4.956

Review 4.  Overview of the structure-based non-genomic effects of the nuclear receptor RXRα.

Authors:  Liqun Chen; Lingjuan Wu; Linyan Zhu; Yiyi Zhao
Journal:  Cell Mol Biol Lett       Date:  2018-08-07       Impact factor: 5.787

5.  3-Alkynylindoles as Building Blocks for the Synthesis of Electronically Tunable Indole-Based Push-Pull Chromophores.

Authors:  Kübra Erden; Cagatay Dengiz
Journal:  J Org Chem       Date:  2022-03-01       Impact factor: 4.354

  5 in total

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