Refining Retinoids with Heteroatoms

Author: Benbrook D.M.

Source: Mini Reviews in Medicinal Chemistry, Volume 2, Number 3, June 2002 , pp. 277-283(7)

Publisher: Bentham Science Publishers

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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 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).

Keywords: retinoid; arotinoid; heteroarotinoid; tazarotene

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557023406160

Publication date: 2002-06-01

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The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.