Author/Authors :
Luc J. Farmer، نويسنده , , Lin Zhi، نويسنده , , Susan Jeong، نويسنده , , E. Adam Kallel، نويسنده , , Glenn 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 were designed and prepared. The lead compound 6a, showed good binding (Kd; 3–7 nM) and transactivation (EC50; 19–24 nM) to the RXR subfamily of retinoid receptors. More importantly, a small variation on the aromatic ring moiety led to 6b, which had less residual RAR agonist activity with RXR binding and potency of 4–5 nM and 5–13 nM, respectively.
