Samuel J. Gillett

Structural basis for the differential RXR & RAR activity of stilbene retinoid analogs

Abstract Retinoids elicit their biological actions by activating nuclear receptors that regulate gene transcription. There are six known retinoid receptors which belong to the retinoic acid receptor (RAR) and retinoid X receptor (RXR) families. We report RXR-active stilbene retinoid analogs and discuss the structural features that impart RAR and RXR activation properties to compounds of this class.

High affinity retinoic acid receptor antagonists: analogs of AGN 193109.

A series of high affinity retinoic acid receptor (RAR) antagonists were prepared based upon the known antagonist AGN 193109 (2). Introduction of various phenyl groups revealed a preference for substitution at the para-position relative to the meta-site. Antagonists with the highest affinities for the RARs possessed hydrophobic groups, however, the presence of polar functionality was also well tolerated.

Synthesis and pharmacological activity of conformationally restricted, acetylenic retinoid analogs

Abstract The biological activity of retinoids are determined by their ability to activate one or more of six nuclear retinoid receptors (RARs and RXRs). We describe rigid, acetylenic retinoids that selectively transactivate through the RARs and RAR/Gg subtypes and demonstrate their potent anti-proliferative activity in the skin.