Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.
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Farmer LJ, Zhi L, Jeong S, Lamph WW, Osburn DL, Croston G, Flatten KS, Heyman RA, Nadzan AM
Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.
Bioorg Med Chem Lett. 2003 Jan 20;13(2):261-4.
- PubMed ID
- 12482435 [ View in PubMed]
- 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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