Refining Retinoids with Heteroatoms

Retinoids are a group of synthetic compounds designed to refine the numerous biological activities of retinoic acid into pharmaceuticals for several diseases, including cancer. Designs that conformationallyrestricted the rotation of the structures resulted in arotinoids that were biologically active, but with increased toxicity. Incorporation of a heteroatom in one cyclic ring of the arotinoid structures drastically reduced the toxicity, while retaining biological activity. Clinical trials of a heteroarotinoid, Tazarotene, confirmed the improved chemotherapeutic ratio (efficacy / toxicity).