SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms

Abby Ho, Yang eon Kim, Hyo Sung Lee, Kedra Cyrus, Sun Hee Baek, Kyung Bo Kim

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


The major estrogen metabolite 2-methoxyestradiol (2ME) has been shown to target tumor cells without severe side effects and is currently being evaluated in clinical trials for several types of cancer. Despite its promise for use in clinical setting, the mechanism(s) by which 2ME exerts its anti-tumor activity is not clearly defined at this time. Employing organic chemistry tools, we synthesized 2ME analogs with which 2ME affinity column was prepared, enabling us to detect a protein that selectively interacts with 2ME. This 2ME analog will be useful as a probe to identify the biological target(s) of 2ME and study their functions in tumor cells.

Original languageEnglish
Pages (from-to)3383-3387
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number13
StatePublished - Jul 1 2006

Bibliographical note

Funding Information:
We thank Reviewer 1 for his helpful comments on the manuscript. This work was supported by the Kentucky Lung Cancer Research Program-Investigator-Initiated Grant (K.K.).


  • 2-Methoxyestradiol
  • Affinity matrix
  • Anti-tumor estrogen metabolites
  • Biotinylation

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


Dive into the research topics of 'SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms'. Together they form a unique fingerprint.

Cite this