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Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid
Luc J Farmer1, Lin Zhi, Susan Jeong
1Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center Drive, San Diego, CA 92121, USA. farmer@vpharm.com
Bioorganic & Medicinal Chemistry Letters
|December 17, 2002
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.