2. Academic Validation
  3. Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid

Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid

  • Bioorg Med Chem Lett. 2003 Jan 20;13(2):261-4. doi: 10.1016/s0960-894x(02)00924-1.
Luc J Farmer 1,  Lin Zhi,  Susan Jeong,  William W Lamph,  Deborah L Osburn,  Glenn Croston,  Karen S Flatten,  Rich A Heyman,  Alex M Nadzan
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center Drive, San Diego, CA 92121, USA. farmer@vpharm.com
PMID: 12482435 DOI: 10.1016/s0960-894x(02)00924-1
Abstract

A series of novel cyclopropanyl methyl hexadienoic acid retinoids was designed and prepared. These compounds exhibited either selective activity as RXR agonists or pan-agonists on one or more of each of the RAR and RXR isoforms. The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro Cancer cell lines, ME 180 and RPMI 8226.

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