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 conformationally-restricted 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).
Benbrook
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Department of Obstetrics and Gynecology, The University of Oklahoma Health Science Center, P.O. Box 26901, Room WP2470, Oklahoma City, OK 73190, USA. Doris-Benbrook@ouhsc.edu
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D015195:Drug Design; D006801:Humans; D018716:Molecular Mimicry; D018168:Receptors, Retinoic Acid / Q000378:metabolism; D012176:Retinoids / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D018168:Receptors, Retinoic Acid; D012176:Retinoids