SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF POTENT CONFORMATIONALLY RESTRICTED RETINOID-X-RECEPTOR LIGANDS

A series of potent retinoid X receptor (RXR) selective ligands were de signed and prepared. The lead compound 6a, showed good binding (K-d; 3 -7 nM) and transactivation (EC50; 19-24 nM) to the RXR subfamily of re tinoid receptors. More importantly, a small variation on the aromatic ring moiety led to 6b, which had less residual RAR agonist activity wi th RXR binding and potency of 4-5 nM and 5-13 nM, respectively. (C) 19 97 Elsevier Science Ltd.