SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms.
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.
Ho
Abby
A
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, USA.
Kim
Yang-eon
YE
Lee
Hyosung
H
Cyrus
Kedra
K
Baek
Sun-Hee
SH
Kim
Kyung-Bo
KB
D000077584:2-Methoxyestradiol; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004958:Estradiol; D000077584:2-Methoxyestradiol