The endogenous
steroid 2-methoxyestradiol (2-ME) is a metabolite of 17β-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.