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-7 alpha positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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2-Methoxyestradiol
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Aorta
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Cell Division / drug effects
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Cell Line
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Estradiol / analogs & derivatives
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Estradiol / chemical synthesis*
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Estradiol / chemistry
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Estradiol / pharmacology*
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Inhibitory Concentration 50
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Microtubules / drug effects
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Mitosis / drug effects
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Molecular Structure
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Muscle, Smooth, Vascular / cytology
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Muscle, Smooth, Vascular / drug effects
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Rats
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Estradiol
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2-Methoxyestradiol