Protein-degrading enediynes: Library screening of Bergman cycloaromatization products

Citation
Gb. Jones et al., Protein-degrading enediynes: Library screening of Bergman cycloaromatization products, ORG LETT, 2(13), 2000, pp. 1863-1866
Citations number
25
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
ORGANIC LETTERS
ISSN journal
15237060 → ACNP
Volume
2
Issue
13
Year of publication
2000
Pages
1863 - 1866
Database
ISI
SICI code
1523-7060(20000629)2:13<1863:PELSOB>2.0.ZU;2-V
Abstract
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 te mperature- and concentration-dependent degradation of human estrogen recept or a upon cycloaromatization.