Author/Authors :
Luc J. Farmer، نويسنده , , Lin Zhi، نويسنده , , Susan Jeong، نويسنده , , William W. Lamph، نويسنده , , Deborah L. Osburn، نويسنده , , Glenn Croston، نويسنده , , Karen S. Flatten، نويسنده , , Rich A. Heyman، نويسنده , , Alex M. Nadzan، نويسنده ,
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 (RARʹs EC50=17–59 nM; RXRʹs EC50=6–14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226.
