Protein-Degrading Enediynes:  Library Screening of Bergman Cycloaromatization Products

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 recept...

Full description

Saved in:
Bibliographic Details
Published inOrganic letters Vol. 2; no. 13; pp. 1863 - 1866
Main Authors Jones, Graham B, Wright, Justin M, Hynd, George, Wyatt, Justin K, Yancisin, Molly, Brown, Myles A
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 29.06.2000
Amer Chemical Soc
Subjects
Antibiotics, Antineoplastic - chemistry
Antibiotics, Antineoplastic - metabolism
Antibiotics, Antineoplastic - pharmacology
Chemistry
Chemistry, Organic
Combinatorial Chemistry Techniques
Drug Evaluation, Preclinical - methods
Humans
Physical Sciences
Receptors, Estrogen - chemistry
Receptors, Estrogen - drug effects
Receptors, Estrogen - metabolism
Science & Technology
SUPERFAMILY
CLEAVAGE
PHOTOCLEAVAGE
STRATEGY
ESTROGEN-RECEPTOR
Online AccessGet full text

Cover

More Information
Summary: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 α upon cycloaromatization.
Bibliography:Medline
NIH RePORTER
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1523-7060
1523-7052
DOI:10.1021/ol005926q