Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs

Pemmaraju N. Rao; James W. Cessac; Tina L. Tinley; Susan L. Mooberry

doi:10.1016/S0039-128X(02)00066-1

Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs

Pemmaraju N. Rao, James W. Cessac, Tina L. Tinley, Susan L. Mooberry

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

41 Scopus citations

Abstract

The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7α positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.

Original language	English (US)
Pages (from-to)	1079-1089
Number of pages	11
Journal	Steroids
Volume	67
Issue number	13-14
DOIs	https://doi.org/10.1016/S0039-128X(02)00066-1
State	Published - Dec 1 2002
Externally published	Yes

Keywords

2-Methoxyestradiol
Antiangiogenesis
Antimitotic activity
Estrogens
Steroids

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Endocrinology
Pharmacology
Clinical Biochemistry
Organic Chemistry

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abstract = "The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7α positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.",

keywords = "2-Methoxyestradiol, Antiangiogenesis, Antimitotic activity, Estrogens, Steroids",

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AU - Rao, Pemmaraju N.

AU - Cessac, James W.

AU - Tinley, Tina L.

AU - Mooberry, Susan L.

PY - 2002/12/1

Y1 - 2002/12/1

N2 - The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7α positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.

AB - The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7α positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.

KW - 2-Methoxyestradiol

KW - Antiangiogenesis

KW - Antimitotic activity

KW - Estrogens

KW - Steroids

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