title: Protein-degrading enediynes: library screening of Bergman cycloaromatization products.
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.
authors.affiliation: Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry, Northeastern University, 360 Huntington Avenue, 102HT, Boston, Massachusetts 02115, USA.
authors.forename: G B
authors.initials: GB
authors.lastname: Jones
authors.forename: J M
authors.initials: JM
authors.lastname: Wright
authors.forename: G
authors.initials: G
authors.lastname: Hynd
authors.forename: J K
authors.initials: JK
authors.lastname: Wyatt
authors.forename: M
authors.initials: M
authors.lastname: Yancisin
authors.forename: M A
authors.initials: MA
authors.lastname: Brown
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D006801:Humans; D011960:Receptors, Estrogen / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*
chemical_list: D000903:Antibiotics, Antineoplastic; D011960:Receptors, Estrogen