Abstract
The C-cyclopropylalkylamide scaffold was previously identified as a new structural framework for antiestrogens. A second generation library provided three compounds that bind estrogen receptor (ER)alpha. Further screening of this library identified an ERbeta hit and inspired another round of SAR. A new focused library was tested for binding to the ERs, and for effects on the growth of breast cancer cell lines and protein levels of common cell cycle regulators.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Binding, Competitive
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Cell Cycle
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Chemistry, Pharmaceutical / methods*
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Estrogen Receptor beta / chemistry*
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Humans
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Inhibitory Concentration 50
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Ligands
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Models, Chemical
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Protein Binding
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Protein Isoforms
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Structure-Activity Relationship
Substances
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Amides
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Antineoplastic Agents
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Estrogen Receptor beta
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Ligands
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Protein Isoforms