Diana F. Colon

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.

Differential RXR & RAR activity of stilbene retinoid analogs bearing thiazole and imidazole carboxylic acids

Retinoids are hormones which activate two distinct families of nuclear receptors: the retinoic acid receptors (RARα,β,γ) and the retinoid X receptors (RXRα,β,γ). We report thiazole and imidazole substituted stilbene analogs that have RXR specific or pan-agonist activity and discuss the structural features that impart these differential activation properties to compounds of this class.

Synthesis and biological activity of 1,2,3,4-tetrahydroquinoline and 3,4-(1H)-dihydroquinolin-2-one analogs of retinoic acid

Abstract Retinoids are natural and synthetic analogs of the hormone retinoic acid. Retinoids are currently being investigated clinically as drugs in several areas, including dermatology and oncology. We report the synthesis and biological activity of a new series of potent, RAR-specific retinoids substituted with a 1,2,3,4-tetrahydroquinoline or a 3,4-(1H)-dihydroquinolin-2-one group.