Abstract
The identification of agents with specific antiproliferative or cytostatic activity against endothelial cells has significant value for the treatment of pathologies associated with angiogenesis, including solid tumors. Here, we describe a novel substituted dibenzo[b,d]pyran-6-one scaffold, exemplified by structures 9a and 10, and report preliminary in vitro activity data indicating that this scaffold is a promising lead for the development of specific inhibitors of endothelial cell proliferation.
MeSH terms
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2-Methoxyestradiol
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Angiogenesis Inhibitors / chemical synthesis*
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Angiogenesis Inhibitors / chemistry
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Angiogenesis Inhibitors / pharmacology
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Binding, Competitive
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Cell Division / drug effects
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Computer Simulation
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Endothelium, Vascular / cytology
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Endothelium, Vascular / drug effects*
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Estradiol / analogs & derivatives
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Estradiol / chemistry
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Estradiol / pharmacology
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Humans
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Models, Molecular
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Pyrans / chemical synthesis*
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Pyrans / chemistry
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Pyrans / pharmacology
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Receptors, Estrogen / metabolism
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Structure-Activity Relationship
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Tumor Cells, Cultured
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Umbilical Veins / cytology
Substances
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Angiogenesis Inhibitors
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Pyrans
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Receptors, Estrogen
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Estradiol
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2-Methoxyestradiol