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

被引：13
|
作者：
Ho, Abby [1 ]
Kim, Yang-eon [1 ]
Lee, Hyosung [1 ]
Cyrus, Kedra [1 ]
Baek, Sun-Hee [1 ]
Kim, Kyung-Bo [1 ]
机构：
[1] Univ Kentucky, Dept Pharmaceut Sci, Coll Pharm, Lexington, KY 40506 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 13期
关键词：
2-methoxyestradiol; affinity matrix; biotinylation; antitumor estrogen metabolites;
D O I：
10.1016/j.bmcl.2006.04.030
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3383 / 3387
页数：5
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