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Synthetic 2-methoxyestradiol derivatives: structure-activity relationships
Jean-François Peyrat1, Jean-Daniel Brion, Mouad Alami
1Univ Paris-Sud, CNRS, BioCIS - UMR 8076, LabEx LERMIT, Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, 5 rue J.-B. Clement, Châtenay-Malabry, F-92296, France. jean-francois.peyrat@u-psud.fr
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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