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Protein-degrading enediynes: library screening of Bergman cycloaromatization products
G B Jones1, J M Wright, G Hynd
1Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry, Northeastern University, 360 Huntington Avenue, 102HT, Boston, Massachusetts 02115, USA.
Organic Letters
|July 13, 2000
Abstract:
[structure: see text] A screening method based on Bergman cycloaromatization products was applied to a compact library of estrogenic-enediyne hybrids. An enediyne candidate identified from the screen was subsequently synthesized, and it induced temperature- and concentration-dependent degradation of human estrogen receptor alpha upon cycloaromatization.