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PubMed · 12370069

Refining retinoids with heteroatoms.

D M Benbrook
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Abstract

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).

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AnimalsAntineoplastic AgentsDrug DesignHumansMolecular MimicryReceptors, Retinoic AcidRetinoidsStructure-Activity RelationshipJournal ArticleReview

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D M Benbrook. 2002. Refining retinoids with heteroatoms.. https://doi.org/10.2174/1389557023406160

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