Benbrook D M
Department of Obstetrics and Gynecology, The University of Oklahoma Health Science Center, P.O. Box 26901, Room WP2470, Oklahoma City, OK 73190, USA.
Mini Rev Med Chem. 2002 Jun;2(3):277-83. doi: 10.2174/1389557023406160.
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).
类视黄醇是一类合成化合物，旨在将视黄酸的多种生物活性提炼成用于治疗包括癌症在内的多种疾病的药物。对结构旋转进行构象限制的设计产生了具有生物活性但毒性增加的芳维甲酸类化合物。在芳维甲酸类化合物结构的一个环中引入杂原子可大幅降低毒性，同时保留生物活性。一种杂芳维甲酸类化合物他扎罗汀的临床试验证实了化疗指数（疗效/毒性）得到改善。
