Author/Authors :
Luc J. Farmer، نويسنده , , Susan Jeong، نويسنده , , E. Adam Kallel، نويسنده , , Stacie S. Canan Koch، نويسنده , , Glenn E. Croston، نويسنده , , Karen S. Flatten، نويسنده , , Rich A. Heyman، نويسنده , , Alex M. Nadzan، نويسنده ,
Abstract :
A series of potent retinoid X receptor (RXR) selective ligands was designed and prepared. The lead compound 7a showed good binding (Ki; 20–50 nM) and transactivation (EC50; 40–50 nM) to the RXR subfamily of retinoid receptors. More importantly, small variations in the geometry of the cyclopentane ring moiety led to 9, one of the most potent RXR agonists to date (Ki: 3–8 nM; EC50: 3–4 nM).
