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Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships

[ Vol. 19 , Issue. 24 ]


Jean-Francois Peyrat, Jean-Daniel Brion and Mouad Alami   Pages 4142 - 4156 ( 15 )


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


Univ Paris-Sud, CNRS, BioCIS-UMR 8076, LabEx LERMIT, Laboratoire de Chimie Therapeutique, Faculte de Pharmacie, 5 rue J.-B. Clement, Chatenay-Malabry, F-92296, France.

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