Synthesis and Pharmacological Effects of the Anti-Cancer Agent 2-Methoxyestradiol
Synthesis and Pharmacological Effects of the Anti-Cancer Agent 2-Methoxyestradiol
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DOI：
10.2174/1381612821666151002112511
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发表时间：
2015-01-01
影响因子：
3.1
通讯作者：
Hansen, Trond Vidar
中科院分区：
文献类型：
--
作者：
Solum, Eirik Johansson;Akselsen, Oyvind W.;Hansen, Trond Vidar
内源性类固醇2-甲氧基雌二醇（2-ME）是17 β-雌二醇的代谢产物，其生物合成已得到充分证实。此外，2-ME也是由雌酮生物合成的。多年来，2-ME被认为是一种无活性的代谢产物，没有任何有趣的生物活性。自20世纪80年代后期以来，许多生物学和药理学研究表明，2-ME具有有趣的抗癌作用，而没有任何不良的雌激素活性。特别是，鉴于基于2-ME的新抗癌药物的开发，2-ME所表现出的抗血管作用和抗血管生成活性具有极大的兴趣和重要性。已经启动了使用类固醇2-ME的几个临床试验开发项目。此外，基于所报道的2-ME的许多药理活性，而且由于对内源性甾族化合物的全合成和半合成的普遍兴趣，几个从事有机合成的研究小组已经制备了这种甾族化合物。本文综述了2-ME的抗癌作用、临床试验结果和合成研究进展。
The endogenous steroid 2-methoxyestradiol (2-ME) is a metabolite of 17 beta-estradiol and its biosynthesis is well established. Moreover, 2-ME is also biosynthesized from estrone. For several years, 2-ME was perceived as an inactive metabolite devoid of any interesting biological activities. Since the late 1980s, a number of biological and pharmacological studies have revealed that 2-ME possesses interesting anti-cancer effects without any undesirable estrogen activity. In particular, the anti-vascular effects and anti-angiogenic activities that 2-ME exhibit, are of great interest and importance, in view of the development of new anti-cancer drugs based on 2-ME. Several clinical trial development programs have been initiated using the steroid 2-ME. In addition, based on the many pharmacological activities reported for 2-ME, but also due to the general interest in total and semi-synthesis of endogenous steroids, several research groups working with organic synthesis have prepared this steroid. Herein, the anti-cancer effects, the results from the clinical trial development programs and the synthetic studies towards 2-ME, are reviewed.