RESUMEN

Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the position of fluorination, and improvement in pharmacological profile was demonstrated in some cases.

Asunto(s)

Compuestos de Flúor/síntesis química , Compuestos de Flúor/metabolismo , Receptores de Ácido Retinoico/metabolismo , Factores de Transcripción/metabolismo , Tretinoina/síntesis química , Tretinoina/metabolismo , Animales , Diseño de Fármacos , Compuestos de Flúor/farmacología , Masculino , Ratones , Ratones Endogámicos ICR , Receptores X Retinoide , Retinoides/síntesis química , Retinoides/metabolismo , Retinoides/farmacología , Tretinoina/farmacología