Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships

Author(s): Jean-Francois Peyrat, Jean-Daniel Brion, Mouad Alami.

Journal Name: Current Medicinal Chemistry

Volume 19 , Issue 24 , 2012

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Abstract:

— 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.

Keywords: — 2-Methoxyestradiol, antiproliferative activity, antimitotic activity, apoptotic activity, antiangiogenesis, anticancer agents, structure-activity relationships, homologation, aromatization, ethynyl groups.

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Article Details

VOLUME: 19
ISSUE: 24
Year: 2012
Page: [4142 - 4156]
Pages: 15
DOI: 10.2174/092986712802430072
Price: $58

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