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

Producción científica: Article › revisión exhaustiva

12 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	3383-3387
Número de páginas	5
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	16
N.º	13
DOI	https://doi.org/10.1016/j.bmcl.2006.04.030
Estado	Published - jul 1 2006

Nota bibliográfica

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.).

Financiación

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.).

Financiadores
Kentucky Lung Cancer Research Association

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

Good health and well being

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2006.04.030

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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",

month = jul,

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

language = "English",

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pages = "3383--3387",

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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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UR - https://www.scopus.com/pages/publications/33646838414#tab=citedBy

U2 - 10.1016/j.bmcl.2006.04.030

DO - 10.1016/j.bmcl.2006.04.030

M3 - Article

C2 - 16650989

AN - SCOPUS:33646838414

SN - 0960-894X

VL - 16

SP - 3383

EP - 3387

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

ER -

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

Resumen

Nota bibliográfica

Financiación

ODS de las Naciones Unidas

ASJC Scopus subject areas

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