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.
Current Medicinal Chemistry
Title:Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships
Volume: 19 Issue: 24
Author(s): Jean-Francois Peyrat, Jean-Daniel Brion and Mouad Alami
Affiliation:
Keywords: — 2-Methoxyestradiol, antiproliferative activity, antimitotic activity, apoptotic activity, antiangiogenesis, anticancer agents, structure-activity relationships, homologation, aromatization, ethynyl groups.
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.
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Cite this article as:
Peyrat Jean-Francois, Brion Jean-Daniel and Alami Mouad, Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships, Current Medicinal Chemistry 2012; 19 (24) . https://dx.doi.org/10.2174/092986712802430072
DOI https://dx.doi.org/10.2174/092986712802430072 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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