Design, synthesis and structure-activity relationship of novel RXR-selective modulators

Pierre-Yves Michellys; Jennifer D'Arrigo; Timothy A Grese; Donald S Karanewsky; Mark D Leibowitz; Dale A Mais; Christopher M Mapes; Anne Reifel-Miller; Deepa Rungta; Marcus F Boehm

doi:10.1016/j.bmcl.2003.12.089

Design, synthesis and structure-activity relationship of novel RXR-selective modulators

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1593-8. doi: 10.1016/j.bmcl.2003.12.089.

Authors

Pierre-Yves Michellys¹, Jennifer D'Arrigo, Timothy A Grese, Donald S Karanewsky, Mark D Leibowitz, Dale A Mais, Christopher M Mapes, Anne Reifel-Miller, Deepa Rungta, Marcus F Boehm

Affiliation

¹ Department of Medicinal Chemistry, Ligand Pharmaceuticals Incorporated, 10275 Science Center Drive, San Diego, CA 92121, USA. pmichellys@gnf.org

PMID: 15006411
DOI: 10.1016/j.bmcl.2003.12.089

Abstract

The synthesis and in vitro characterization of novel RXR-selective ligands possessing various substituted 1-benzofuran or 1-benzothiophene moieties are described.

MeSH terms

Drug Design*
Protein Binding / physiology
Receptors, Retinoic Acid / metabolism*
Retinoid X Receptors
Structure-Activity Relationship
Transcription Factors / metabolism*
Tretinoin / analogs & derivatives*
Tretinoin / metabolism*

Substances

Receptors, Retinoic Acid
Retinoid X Receptors
Transcription Factors
Tretinoin