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Title: Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

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 LXR{alpha} will be disclosed.

Authors:
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Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1005519
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorg. Med. Chem. Lett.; Journal Volume: 19; Journal Issue: (4) ; 02, 2009
Country of Publication:
United States
Language:
ENGLISH
Subject:
36 MATERIALS SCIENCE; AMINES; ARTERIOSCLEROSIS; CRYSTAL STRUCTURE; HORMONES; INDOLES; INFLAMMATION; LIVER; SYNTHESIS

Citation Formats

Washburn, David G., Hoang, Tram H., Campobasso, Nino, Smallwood, Angela, Parks, Derek J., Webb, Christine L., Frank, Kelly A., Nord, Melanie, Duraiswami, Chaya, Evans, Christopher, Jaye, Michael, Thompson, Scott K., GSKNC), and GSKPA). Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. United States: N. p., 2009. Web. doi:10.1016/j.bmcl.2009.01.004.
Washburn, David G., Hoang, Tram H., Campobasso, Nino, Smallwood, Angela, Parks, Derek J., Webb, Christine L., Frank, Kelly A., Nord, Melanie, Duraiswami, Chaya, Evans, Christopher, Jaye, Michael, Thompson, Scott K., GSKNC), & GSKPA). Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. United States. doi:10.1016/j.bmcl.2009.01.004.
Washburn, David G., Hoang, Tram H., Campobasso, Nino, Smallwood, Angela, Parks, Derek J., Webb, Christine L., Frank, Kelly A., Nord, Melanie, Duraiswami, Chaya, Evans, Christopher, Jaye, Michael, Thompson, Scott K., GSKNC), and GSKPA). 2009. "Synthesis and SAR of potent LXR agonists containing an indole pharmacophore". United States. doi:10.1016/j.bmcl.2009.01.004.
@article{osti_1005519,
title = {Synthesis and SAR of potent LXR agonists containing an indole pharmacophore},
author = {Washburn, David G. and Hoang, Tram H. and Campobasso, Nino and Smallwood, Angela and Parks, Derek J. and Webb, Christine L. and Frank, Kelly A. and Nord, Melanie and Duraiswami, Chaya and Evans, Christopher and Jaye, Michael and Thompson, Scott K. and GSKNC) and GSKPA)},
abstractNote = {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 LXR{alpha} will be disclosed.},
doi = {10.1016/j.bmcl.2009.01.004},
journal = {Bioorg. Med. Chem. Lett.},
number = (4) ; 02, 2009,
volume = 19,
place = {United States},
year = 2009,
month = 3
}
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