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2000
Volume 19, Issue 24
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

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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/content/journals/cmc/10.2174/092986712802430072
2012-08-01
2025-06-01
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