2. Academic Validation
  3. Design and synthesis of novel RXR-selective modulators with improved pharmacological profile

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

  • Bioorg Med Chem Lett. 2003 Nov 17;13(22):4071-5. doi: 10.1016/j.bmcl.2003.08.048.
Pierre-Yves Michellys 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Ligand Pharmaceuticals Incorporated, 10275 Science Center Drive, San Diego, CA 92121, USA. [email protected]
PMID: 14592510 DOI: 10.1016/j.bmcl.2003.08.048
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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