Univ Paris-Sud, CNRS, BioCIS - UMR 8076, LabEx LERMIT, Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, 5 rue J.-B. Clement, Châtenay-Malabry, F-92296, France.
Curr Med Chem. 2012;19(24):4142-56. doi: 10.2174/092986712802430072.
2-Methoxyestradiol (2ME2), a natural metabolite of estradiol which has no estrogenic activity, is a potent antitumor and anti-angiogenic compound, currently undergoing clinical trials for treatment of a variety of cancers. In the last two decades, an ever increasing number of synthetic 2-methoxyestradiol analogues have been reported. Structural changes include A/B/C/D-rings modification, homologation, aromatization, and introduction of various substituents on C-2 position along with substitution of alkyl and ethynyl groups for the 17-hydroxy function. In this review, an attempt has been made to compile the structure-activity relationships of various synthesized 2-methoxyestradiol analogues.
2-甲氧基雌二醇（2ME2）是雌二醇的一种天然代谢物，没有雌激素活性，是一种有效的抗肿瘤和抗血管生成化合物，目前正在进行临床试验，用于治疗多种癌症。在过去的二十年中，报道了越来越多的合成 2-甲氧基雌二醇类似物。结构变化包括 A/B/C/D 环修饰、同系化、芳构化以及在 C-2 位置引入各种取代基，同时取代 17-羟基功能的烷基和乙炔基。在这篇综述中，尝试总结了各种合成 2-甲氧基雌二醇类似物的结构-活性关系。
