2-Methoxyestradiol - a unique blend of activities generating a new class of anti-tumour/anti-inflammatory agents

Tara E Sutherland, Robin L Anderson, Richard A Hughes, Emile Altmann, Michael Schuliga, James Ziogas, Alastair G Stewart

Research output: Contribution to journalArticlepeer-review

80 Citations (Scopus)


The estradiol metabolite, 2-methoxyestradiol (2MEO), is currently being evaluated in Phase II clinical trials for the treatment of solid tumours and is undergoing preclinical evaluation for inflammatory conditions. The anti-proliferative/cytotoxic/pro-apoptotic effects on tumour and endothelial cells have conferred potential on this metabolite for a synergistic impact on tumour growth. Exploitation of this synergy of 2MEO has previously required the combination of well-established cytotoxic agents with newer anti-angiogenic agents. This article reviews the pharmacology of 2MEO and describes the limitations inherent in its residual estrogen receptor affinity. The extent to which the metabolite 2MEO embodies an optimised therapeutic candidate is discussed. The challenges involved in using rational (3D QSAR-based) drug design to optimise the activity profile of analogues of 2MEO to provide additional members of this new class of anti-tumour/anti-inflammatory drug are also outlined.
Original languageEnglish
Pages (from-to)577-584
Number of pages7
JournalDrug Discovery Today
Issue number13-14
Publication statusPublished - 1 Jul 2007


  • Angiogenesis Inhibitors
  • Animals
  • Anti-Inflammatory Agents
  • Antineoplastic Agents
  • Apoptosis
  • Cell Proliferation
  • Drug Design
  • Estradiol
  • Humans
  • Neoplasms
  • Quantitative Structure-Activity Relationship


Dive into the research topics of '2-Methoxyestradiol - a unique blend of activities generating a new class of anti-tumour/anti-inflammatory agents'. Together they form a unique fingerprint.

Cite this