Protein-degrading enediynes: library screening of Bergman cycloaromatization products.

Org Lett

Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry, Northeastern University, 360 Huntington Avenue, 102HT, Boston, Massachusetts 02115, USA.

Published: June 2000

[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.

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http://dx.doi.org/10.1021/ol005926qDOI Listing

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