Refining Retinoids with Heteroatoms

被引：17

作者：

Benbrook, D. M. ^{[1
]}

机构：

[1] Univ Oklahoma, Hlth Sci Ctr, Dept Obstet & Gynecol, Oklahoma City, OK 73190 USA

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2002年 / 2卷 / 03期

关键词：

D O I：

10.2174/1389557023406160

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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).

引用

页码：277 / 283

页数：7

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