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

doi:10.1016/j.bmcl.2006.04.030

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

Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

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 language	English
Pages (from-to)	3383-3387
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2006.04.030
State	Published - 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.).

Keywords

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2006.04.030

Cite this

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title = "SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms",

abstract = "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.",

keywords = "2-Methoxyestradiol, Affinity matrix, Anti-tumor estrogen metabolites, Biotinylation",

author = "Abby Ho and Kim, {Yang eon} and Lee, {Hyo Sung} and Kedra Cyrus and Baek, {Sun Hee} and Kim, {Kyung Bo}",

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.). ",

year = "2006",

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doi = "10.1016/j.bmcl.2006.04.030",

language = "English",

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T1 - SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms

AU - Ho, Abby

AU - Kim, Yang eon

AU - Lee, Hyo Sung

AU - Cyrus, Kedra

AU - Baek, Sun Hee

AU - Kim, Kyung Bo

N1 - 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.).

PY - 2006/7/1

Y1 - 2006/7/1

N2 - 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.

AB - 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.

KW - 2-Methoxyestradiol

KW - Affinity matrix

KW - Anti-tumor estrogen metabolites

KW - Biotinylation

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U2 - 10.1016/j.bmcl.2006.04.030

DO - 10.1016/j.bmcl.2006.04.030

M3 - Article

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EP - 3387

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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