Literature DB >> 14592510

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

Pierre-Yves Michellys1, Marcus F Boehm, Jyun-Hung Chen, Timothy A Grese, Donald S Karanewsky, Mark D Leibowitz, Sha Liu, Dale A Mais, Christopher M Mapes, Anne Reifel-Miller, Katheen M Ogilvie, Deepa Rungta, Anthony W Thompson, John S Tyhonas, Nathan Yumibe, Robert J Ardecky.   

Abstract

New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their metabolic properties (exposure in IRC male mice) and show a dramatic increase of exposure compared to our reference compound, 3 (LG101506).

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Year:  2003        PMID: 14592510     DOI: 10.1016/j.bmcl.2003.08.048

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.  A rexinoid antagonist increases the hypothalamic-pituitary-thyroid set point in mice and thyrotrope cells.

Authors:  Jennifer S Janssen; Vibha Sharma; Umarani Pugazhenthi; Celia Sladek; William M Wood; Bryan R Haugen
Journal:  Mol Cell Endocrinol       Date:  2011-03-31       Impact factor: 4.102

3.  IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING.

Authors:  Kelly Teske; Premchendar Nandhikonda; Jonathan W Bogart; Belaynesh Feleke; Preetpal Sidhu; Nina Yuan; Joshua Preston; Robin Goy; Lanlan Han; Nicholas R Silvaggi; Rakesh K Singh; Daniel D Bikle; James M Cook; Leggy A Arnold
Journal:  Nucl Receptor Res       Date:  2014

4.  Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).

Authors:  Carl E Wagner; Peter W Jurutka; Pamela A Marshall; Thomas L Groy; Arjan van der Vaart; Joseph W Ziller; Julie K Furmick; Mark E Graeber; Erik Matro; Belinda V Miguel; Ivy T Tran; Jungeun Kwon; Jamie N Tedeschi; Shahram Moosavi; Amina Danishyar; Joshua S Philp; Reina O Khamees; Jevon N Jackson; Darci K Grupe; Syed L Badshah; Justin W Hart
Journal:  J Med Chem       Date:  2009-10-08       Impact factor: 7.446

5.  The rexinoid V-125 reduces tumor growth in preclinical models of breast and lung cancer.

Authors:  Lyndsey A Reich; Jessica A Moerland; Ana S Leal; Di Zhang; Sarah Carapellucci; Beth Lockwood; Peter W Jurutka; Pamela A Marshall; Carl E Wagner; Karen T Liby
Journal:  Sci Rep       Date:  2022-01-07       Impact factor: 4.379

  5 in total

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