Protein-degrading enediynes: library screening of Bergman cycloaromatization products.
[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.
Jones
G B
GB
Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry, Northeastern University, 360 Huntington Avenue, 102HT, Boston, Massachusetts 02115, USA.
Wright
J M
JM
Hynd
G
G
Wyatt
J K
JK
Yancisin
M
M
Brown
M A
MA
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*
D000903:Antibiotics, Antineoplastic; D011960:Receptors, Estrogen