The endogenous steroid 2-methoxyestradiol (2-ME) is a metabolite of 17-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,
Keywords: Steroid, 2-methoxyestradiol, anti-cancer effects, anti-vascular effects, anti-angiogenic activities, tubulin inhibition, clinical trials,
total synthesis, regioselectivity.
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